Autophagy

Autophagy Products

  • All (305)
  • Autophagy Inhibitors (66)
  • Autophagy Activators (219)
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  • Autophagy Modulators (16)
  • New Autophagy Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1078 MK-2206 2HCl MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.
Nat Cancer, 2024,
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
Nat Commun, 2024, 15(1):2132
S1039 Rapamycin Rapamycin is a specific mTOR inhibitor with IC50 of ~0.1 nM in HEK293 cells.Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator and an immunosuppressant.
Cancer Cell, 2024, S1535-6108(24)00350-7
Drug Resist Updat, 2024, 73:101063
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
S1105 LY294002 LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Signal Transduct Target Ther, 2024, 9(1):109
Signal Transduct Target Ther, 2024, 9(1):109
Nat Genet, 2024, 10.1038/s41588-024-01891-8
S2673 Trametinib (GSK1120212) Trametinib (GSK1120212, JTP-74057) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib activates autophagy and induces apoptosis.
Nature, 2024, 629(8013):927-936
Cell, 2024, 187(3):712-732.e38
Cell, 2024, S0092-8674(24)00825-0
S1060 Olaparib (AZD2281) Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Cell, 2024, 187(4):945-961.e18
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Cancer Cell, 2024, 42(4):535-551.e8
Nat Commun, 2024, 15(1):2581
Nat Commun, 2024, 15(1):987
S1049 Y-27632 2HCl Y-27632 2HCl is a selective ROCK1 and ROCK2 inhibitor with a Ki of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Neural Regen Res, 2025, 20(1):242-252
Nature, 2024, 627(8004):594-603
Nature, 2024, 628(8009):818-825
S1013 Bortezomib Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.
Cell, 2024, 187(18):4905-4925.e24
Cell, 2024, S0092-8674(24)00315-5
Cell, 2024, S0092-8674(24)00653-6
S2767 3-MA (3-Methyladenine) 3-MA (3-Methyladenine) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. Solutions are unstable and should be fresh-prepared.
Bioact Mater, 2024, 32:277-291
Nat Commun, 2024, 15(1):1669
Adv Sci (Weinh), 2024, 11(32):e2400952
S1263 Laduviglusib (CHIR-99021) Laduviglusib (CHIR-99021, CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.
Cell Stem Cell, 2024, S1934-5909(24)00256-X
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Protein Cell, 2024, pwae031
S1120 Everolimus Everolimus is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.
Cell, 2024, 187(3):712-732.e38
Cell, 2024, 187(3):712-732.e38
Kidney Int, 2024, S0085-2538(24)00627-6
S1102 U0126-EtOH U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.
MedComm (2020), 2024, 5(5):e525
Int J Biol Sci, 2024, 20(6):2202-2218
Cell Death Dis, 2024, 15(1):31
S1025 Gefitinib Gefitinib is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Nature, 2024, 631(8020):424-431
Signal Transduct Target Ther, 2024, 9(1):65
Nat Genet, 2024, 10.1038/s41588-024-01948-8
S1166 Cisplatin Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
Int J Mol Med, 2025, 55(1)17
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
Nat Commun, 2024, 15(1):5775
S1267 Vemurafenib (PLX4032) Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.
Cell, 2024, 187(14):3652-3670.e40
Nat Commun, 2024, 15(1):4108
Nat Commun, 2024, 15(1):4108
S2924 Laduviglusib (CHIR-99021) HCl Laduviglusib (CHIR-99021; CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.
Nature, 2024, 10.1038/s41586-024-07706-4
Nature, 2024, 632(8027):1073-1081
Cell, 2024, 187(3):692-711.e26
S1378 Ruxolitinib Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Nat Commun, 2024, 15(1):2503
Nat Commun, 2024, 15(1):8663
Nat Commun, 2024, 15(1):2989
S1023 Erlotinib HCl Erlotinib HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Cell Discov, 2024, 10(1):39
J Extracell Vesicles, 2024, 13(7):e12494
Cell Mol Gastroenterol Hepatol, 2024, S2352-345X(24)00119-X
S7786 Erlotinib Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
Signal Transduct Target Ther, 2024, 9(1):65
Mol Cancer, 2024, 23(1):48
Nat Commun, 2024, 15(1):2742
S8048 Venetoclax (ABT-199) Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.
Nature, 2024,
Nat Immunol, 2024, 10.1038/s41590-024-01952-4
J Hematol Oncol, 2024, 17(1):85
S1047 Vorinostat (SAHA) Vorinostat (SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Cell Rep, 2024, 43(1):113575
NPJ Precis Oncol, 2024, 8(1):52
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
S1021 Dasatinib Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
Nature, 2024, 627(8003):407-415
Nature, 2024, 10.1038/s41586-024-07079-8
Mol Cancer, 2024, 23(1):240
S1250 Enzalutamide Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Acta Pharm Sin B, 2024, 14(6):2685-2697
Cell Rep Med, 2024, 5(2):101388
Cancer Lett, 2024, 597:217068
S7397 Sorafenib Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
J Hematol Oncol, 2024, 17(1):78
Cell Rep Med, 2024, S2666-3791(24)00201-5
J Exp Clin Cancer Res, 2024, 43(1):143
S7306 Dorsomorphin 2HCl Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.
Nat Commun, 2024, 15(1):4124
Nat Commun, 2024, 15(1):4124
Adv Sci (Weinh), 2024, 11(4):e2304987
S2111 Lapatinib Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
Drug Resist Updat, 2024, 73:101066
J Extracell Vesicles, 2024, 13(7):e12494
Cancer Lett, 2024, 593:216968
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
J Clin Invest, 2024, 134(18)e179860
Haematologica, 2024, 109(6):1713-1725
S1065 Pictilisib (GDC-0941) Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.
Nature, 2024, 10.1038/s41586-024-08031-6
Nat Genet, 2024, 10.1038/s41588-024-01948-8
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
S1068 Crizotinib Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Cancer Discov, 2024, OF1-OF20.
Nat Commun, 2024, 15(1):1009
Nat Commun, 2024, 15(1):51
S7840 Dorsomorphin Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For cell testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.
Nat Commun, 2024, 15(1):8547
J Clin Invest, 2024, 134(22)e181314
Nucleic Acids Res, 2024, gkae707
S1053 Entinostat (MS-275) Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Nat Commun, 2024, 15(1):4739
Nat Commun, 2024, 15(1):8044
J Clin Invest, 2024, 134(6)e171063
S1150 Paclitaxel Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy.
Bioact Mater, 2025, 43:67-81
Nat Commun, 2024, 15(1):2503
Nat Commun, 2024, 15(1):2089
S1413 Bafilomycin A1 (Baf-A1) Bafilomycin A1(Baf-A1) is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.
Nature, 2024, 626(8000):874-880
Nature, 2024, 626(8000):874-880
Cell, 2024, 187(21):6055-6070.e22
S1030 Panobinostat (LBH589) Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Nat Commun, 2024, 15(1):4450
Nat Commun, 2024, 15(1):5209
Emerg Microbes Infect, 2024, 13(1):2327371
S1011 Afatinib Afatinib inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
Cell, 2024, 187(3):712-732.e38
Cell, 2024, S0092-8674(24)00825-0
Signal Transduct Target Ther, 2024, 9(1):65
S7110 (+)-JQ1 (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Nat Immunol, 2024, 25(9):1580-1592
Gastroenterology, 2024, S0016-5085(24)00062-3
ACS Nano, 2024, 18(39):26614-26630
S2215 DAPT DAPT is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.
Nat Biotechnol, 2024, 10.1038/s41587-024-02386-x
Nat Commun, 2024, 15(1):9529
J Clin Invest, 2024, 134(18)e179860
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Nat Commun, 2024, 15(1):1041
Cell Rep Med, 2024, 5(3):101471
Redox Biol, 2024, 72:103137
S1002 ABT-737 ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.
Gastroenterology, 2024, S0016-5085(24)00062-3
Nat Commun, 2024, 15(1):830
Nat Commun, 2024, 15(1):1041
S1092 KU-55933 KU-55933 is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
Nature, 2024, 629(8011):443-449
Nature, 2024, 629(8011):443-449
Cell, 2024, 187(20):5698-5718.e26
S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nature, 2024, 10.1038/s41586-024-07990-0
Nat Commun, 2024, 15(1):451
Nat Commun, 2024, 15(1):4926
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
Nat Cancer, 2024,
Nat Commun, 2024, 15(1):1300
Nat Commun, 2024, 15(1):7455
S1225 Etoposide Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis.
Nature, 2024, 635(8037):201-209
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
Nat Commun, 2024, 15(1):9181
S2475 Imatinib Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Nat Biomed Eng, 2024, 10.1038/s41551-024-01204-8
Cell Rep Med, 2024, S2666-3791(24)00201-5
Elife, 2024, 12RP92324
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Leukemia, 2024, 38(5):969-980
Clin Transl Med, 2024, 14(5):e1703
Clin Transl Med, 2024, 14(5):e1703
S2226 Idelalisib (CAL-101) Idelalisib (CAL-101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.
Cancer Immunol Res, 2024, 10.1158/2326-6066.CIR-23-1092
Transl Oncol, 2024, 43:101857
J Cell Commun Signal, 2024, 18(1):e12017
S1040 Sorafenib tosylate Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Nature, 2024, 629(8013):927-936
Cell Mol Life Sci, 2024, 81(1):238
J Transl Med, 2024, 22(1):593
S1555 AZD8055 AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.
Gastroenterology, 2024, S0016-5085(24)00062-3
Nat Commun, 2024, 15(1):2581
Nat Commun, 2024, 15(1):7675
S1714 Gemcitabine Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.
Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
Drug Resist Updat, 2024, 74:101079
Nat Commun, 2024, 15(1):1287
S1026 Imatinib Mesylate Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
Mol Cancer, 2024, 23(1):240
Cell Rep, 2024, 43(3):113811
JCI Insight, 2024, 9(10):e162449.
S1004 Veliparib (ABT-888) Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Cell Rep, 2024, 43(5):114205
S8037 Necrostatin-1 Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
Mol Cancer, 2024, 23(1):113
Mil Med Res, 2024, 11(1):22
Redox Biol, 2024, 75:103270
S7781 Sunitinib Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Cell Rep Med, 2024, S2666-3791(24)00201-5
Pharmaceuticals (Basel), 2024, 17(1)77
Heliyon, 2024, 10(3):e24779
S2827 Torin 1 Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.
Mol Cell, 2024, S1097-2765(24)00832-3
Mol Cell, 2024, 84(8):1527-1540.e7
EMBO J, 2024,
S2853 Carfilzomib (PR-171) Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
Nature, 2024, 626(8000):874-880
J Hematol Oncol, 2024, 17(1):85
Nat Commun, 2024, 15(1):2207
S1224 Oxaliplatin Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
Mol Cancer, 2024, 23(1):186
Mol Cancer, 2024, 23(1):23
Gastroenterology, 2024, S0016-5085(24)00062-3
S1490 Ponatinib Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
Int J Biol Sci, 2024, 20(9):3412-3425
Cell Rep, 2024, 43(3):113932
Elife, 2024, 12RP92324
S1178 Regorafenib Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.
Nat Med, 2024, 10.1038/s41591-024-02824-y
Nature, 2024, 629(8011):450-457
Cell Rep Med, 2024, S2666-3791(24)00201-5
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Nat Commun, 2024, 15(1):1642
Cancer Lett, 2024, 604:217258
Phytomedicine, 2024, 135:156053
S1237 TMZ(Temozolomide) TMZ(Temozolomide) is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity.
Cell Discov, 2024, 10(1):39
Cell Death Dis, 2024, 15(3):205
NPJ Precis Oncol, 2024, 8(1):59
S5243 Ruxolitinib Phosphate Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Virol J, 2024, 21(1):23
Int J Mol Sci, 2023, 24(7)6228
Front Oncol, 2023, 13:1043694
S1130 Sepantronium Bromide (YM155) Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.
Cell Commun Signal, 2024, 22(1):440
Sci Rep, 2024, 14(1):7604
Adv Sci (Weinh), 2023, 10(25):e2301753
S1129 SRT1720 HCl SRT1720 HCl is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3. SRT1720 induces autophagy.
Int J Mol Sci, 2024, 25(17)9707
Int Immunopharmacol, 2024, 143(Pt 2):113521
Mol Pain, 2024, 20:17448069241232349
S1077 SB202190 SB202190 is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Nat Commun, 2024, 15(1):4124
Nat Commun, 2024, 15(1):5874
Nat Commun, 2024, 15(1):4124
S1149 Gemcitabine HCl Gemcitabine HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.
Int J Biol Sci, 2024, 20(4):1389-1409
Phytomedicine, 2024, 155377
NPJ Precis Oncol, 2024, 8(1):246
S7810 Afatinib Dimaleate Afatinib Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.
Cell, 2024, 187(3):712-732.e38
Signal Transduct Target Ther, 2024, 9(1):153
J Invest Dermatol, 2024, S0022-202X(23)03210-4
S1582 H 89 2HCl H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy.
Nat Commun, 2024, 15(1):8887
J Extracell Vesicles, 2024, 13(4):e12426
J Extracell Vesicles, 2024, 13(4):e12426
S1191 Fulvestrant Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.
Cancer Lett, 2024, 593:216968
Cell Death Dis, 2024, 15(8):590
Cell Death Dis, 2024, 15(7):480
S2449 Forskolin (Colforsin) Forskolin (Colforsin) is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types, commonly used to raise levels of cAMP in the study and research of cell physiology. Forskolin also activates PXR and FXR activity. Forskolin stimulates autophagy.
Circulation, 2024, 149(18):1435-1456
Cell Stem Cell, 2024, S1934-5909(24)00048-1
Sci Bull (Beijing), 2024, S2095-9273(24)00799-0
S1033 Nilotinib Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Nat Commun, 2024, 15(1):651
Nat Commun, 2024, 15(1):2089
Elife, 2024, 12RP92324
S2248 Silmitasertib (CX-4945) Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.
Diabetologia, 2024, 10.1007/s00125-024-06128-1
Biomed Pharmacother, 2024, 180:117499
Front Immunol, 2024, 15:1393485
S1141 Tanespimycin (17-AAG) Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
Cell, 2024, S0092-8674(24)00583-X
Cell, 2024, S0092-8674(24)00583-X
Theranostics, 2024, 14(6):2442-2463
S1014 Bosutinib Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
Elife, 2024, 12RP92324
Front Immunol, 2024, 15:1425670
PLoS Pathog, 2024, 20(7):e1012170
S1048 Tozasertib (VX-680) Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.
Cell Death Dis, 2024, 15(1):56
Cell Rep, 2024, 43(9):114739
Elife, 2024, 12RP92324
S1786 Verteporfin Verteporfin is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis.
Acta Pharm Sin B, 2024, 14(3):1222-1240
Bone Res, 2024, 12(1):12
Cancer Lett, 2024, 587:216692
S6999 Chloroquine Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Signal Transduct Target Ther, 2024, 9(1):65
Mol Cancer, 2024, 23(1):240
Bioact Mater, 2024, 32:277-291
S2704 LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocks autophagy and induces apoptosis.
Cell Mol Life Sci, 2024, 81(1):173
Cell Mol Life Sci, 2024, 81(1):173
Int J Mol Sci, 2024, 25(2)959
S1230 Flavopiridol (Alvocidib) Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.
Nat Commun, 2024, 15(1):5151
Nat Commun, 2024, 15(1):8539
Nat Commun, 2024, 15(1):35
S2929 Pifithrin-α (PFTα) HBr Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).
Cell Death Differ, 2024, 31(8):999-1012
Int J Biol Sci, 2024, 20(6):2008-2026
Cell Mol Life Sci, 2024, 81(1):101
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
EMBO J, 2024, 10.1038/s44318-024-00244-9
EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9
CNS Neurosci Ther, 2024, 30(8):e14913
S1241 Vincristine sulfate Vincristine sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.
Nat Commun, 2024, 15(1):4513
Nat Commun, 2024, 15(1):4739
iScience, 2024, 27(1):108667
S1057 Obatoclax Mesylate (GX15-070) Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Emerg Microbes Infect, 2022, 1-29
Cancers (Basel), 2022, 14(22)5602
S1046 Vandetanib Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
Front Pharmacol, 2024, 15:1345070
Front Pharmacol, 2024, 15:1345070
S1122 Mocetinostat (MGCD0103) Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.
Dev Cell, 2024, S1534-5807(24)00326-5
J Invest Dermatol, 2024, S0022-202X(23)03210-4
Clin Epigenetics, 2024, 16(1):13
S1069 Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Cell Commun Signal, 2024, 22(1):397
Sci Adv, 2024, 10(8):eadk3663
bioRxiv, 2024, 10.1101/2024.01.16.575190
S1782 Azacitidine (5-Azacytidine) Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.
J Hematol Oncol, 2024, 17(1):85
Nat Commun, 2024, 15(1):7360
Nat Commun, 2024, 15(1):4739
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Cancers (Basel), 2024, 16(13)2447
bioRxiv, 2024, 2024.02.19.581073
J Transl Med, 2023, 21(1):89
S2775 Nocodazole Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
Nat Commun, 2024, 15(1):9771
Nucleic Acids Res, 2024, gkae605
S4430 Hydroxychloroquine (HCQ) Sulfate Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Redox Biol, 2024, 75:103274
Phytomedicine, 2024, 10.1016/j.phymed.2023.155152
Breast Cancer Res, 2024, 26(1):33
S7153 10058-F4 10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 promotes a caspase-3-dependent apoptosis and modulates autophagy.
Cell Metab, 2024, S1550-4131(24)00284-5
Cell Stem Cell, 2024, S1934-5909(24)00041-9
Sci Rep, 2024, 14(1):4060
S1044 Temsirolimus Temsirolimus is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
ACS Nano, 2024, 18(45):31451-31465
Cell Commun Signal, 2024, 22(1):428
iScience, 2024, 27(6):109817
S1085 Belinostat Belinostat is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.
Nat Commun, 2024, 15(1):4739
J Immunother Cancer, 2024, 12(10)e009590
Cell Rep, 2024, 43(1):113575
S2218 Torkinib (PP242) Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and apoptosis.
Mol Cell, 2024, S1097-2765(24)00832-3
Cell Death Dis, 2024, 15(1):48
Mol Oncol, 2024, 10.1002/1878-0261.13716
S7152 C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.
Nat Commun, 2024, 15(1):5209
Cell Commun Signal, 2024, 22(1):117
Antioxidants (Basel), 2024, 13(4)424
S1322 Dexamethasone Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.
Cell Host Microbe, 2024, S1931-3128(24)00005-2
Nat Commun, 2024, 15(1):7991
Nat Commun, 2024, 15(1):1176
S8075 GANT61 GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.
EBioMedicine, 2024, 101:105026
Cell Death Dis, 2024, 15(10):739
Acta Pharm Sin B, 2023, 13(6):2601-2612
S1075 SB216763 SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB216763 activates autophagy.
Sci Rep, 2024, 14(1):11174
SLAS Discov, 2024, 29(8):100191
Leukemia, 2023, 37(8):1611-1625
S8049 Tubastatin A Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
Theranostics, 2024, 14(6):2345-2366
Biomedicines, 2024, 12(6)1203
Life Sci Alliance, 2024, 7(7)e202302384
S5003 Tacrolimus (FK506) Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
Nat Immunol, 2024, 25(5):860-872
Int J Antimicrob Agents, 2024, 63(5):107116
Cell Commun Signal, 2024, 22(1):428
S1950 Metformin HCl Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Nat Commun, 2024, 15(1):1785
J Clin Invest, 2024, e175023
EBioMedicine, 2024, 102:105090
S7007 Binimetinib (MEK162) Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.
Nature, 2024, 629(8013):927-936
Signal Transduct Target Ther, 2024, 9(1):293
Gastroenterology, 2024, S0016-5085(24)00062-3
S2783 Vistusertib (AZD2014) Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
Cell Rep Med, 2023, 4(4):101007
Front Pharmacol, 2023, 14:1158775
Cancers (Basel), 2023, 15(13)3451
S7655 Telaglenastat (CB-839) Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1.
Nat Commun, 2024, 15(1):9820
Nat Commun, 2024, 15(1):5620
EBioMedicine, 2024, 102:105090
S2626 Rabusertib (LY2603618) Rabusertib (LY2603618, IC-83) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
Cell, 2024, 187(14):3652-3670.e40
Mol Cell, 2024, S1097-2765(24)00285-5
Neoplasia, 2024, 57:101038
S1648 Cytarabine Cytarabine is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.
Nat Commun, 2024, 15(1):4739
Nat Commun, 2024, 15(1):9820
Blood Adv, 2024, 8(20):5315-5329
S7307 GSK2606414 GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. GSK2606414 impairs GANT-61 induced autophagy in NB cells with MYCN amplification. GSK2606414 exacerbates ER stress-induced apoptosis in HCT116 cells while reduces the apoptosis in SIL1 KD HeLa cells.
Cell, 2024, 187(14):3652-3670.e40
Autophagy, 2024, 1-22.
Exp Mol Med, 2024, 56(2):408-421.
S1233 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines.
Theranostics, 2024, 14(13):5123-5140
Int J Biol Sci, 2024, 20(6):2323-2338
J Transl Med, 2024, 22(1):649
S8059 Nutlin-3a Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.
EMBO J, 2024, 10.1038/s44318-024-00240-z
J Neuroinflammation, 2024, 21(1):57
Front Immunol, 2024, 15:1374943
S1573 Fasudil HCl Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
J Immunother Cancer, 2024, 12(11)e009805
Sci China Life Sci, 2024, 67(8):1549-1562
CNS Neurosci Ther, 2024, 30(11):e70098
S3012 Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
Cell Rep Med, 2024, S2666-3791(24)00201-5
Biomed Pharmacother, 2024, 180:117468
Transl Psychiatry, 2024, 14(1):166
S7811 MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
Bone Res, 2024, 12(1):15
J Exp Clin Cancer Res, 2024, 43(1):112
Sci Total Environ, 2024, 921:171101
S1274 BX-795 BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively.
EMBO J, 2024, 10.1038/s44318-024-00244-9
PLoS Pathog, 2024, 20(7):e1012170
Vet Microbiol, 2024, 290:109973
S5742 Deferoxamine mesylate Deferoxamine mesylate is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy.Please do not prepare stock solutions with normal saline or PBS, as precipitation may occur.
Mol Cancer, 2024, 23(1):240
Cancer Commun (Lond), 2024, 10.1002/cac2.12608
Adv Sci (Weinh), 2024, 11(40):e2402671
S1017 Cediranib (AZD2171) Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.
Front Oncol, 2024, 14:1302850
Cell Oncol (Dordr), 2023, 46(2):391-407
Cell Oncol (Dordr), 2023, 46(2):391-407
S2180 Ixazomib (MLN2238) Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Ixazomib (MLN2238) induces autophagy. Phase 3.
Sci Rep, 2024, 14(1):18772
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
iScience, 2023, 26(8):107302
S4908 SN-38 SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.
Cell, 2024, 187(20):5698-5718.e26
Nat Commun, 2024, 15(1):2503
Cell Rep Med, 2024, 5(7):101627
S7409 Anisomycin Anisomycin (Flagecidin, Wuningmeisu C) is a bacterial antibiotic isolated from Streptomyces griseolus, which inhibits protein synthesis, and also act as a JNK activator. Anisomycin upregulates autophagy and increases apoptosis.
Theranostics, 2024, 14(4):1561-1582
Research (Wash D C), 2024, 7:0331
Acta Biomater, 2024, S1742-7061(24)00036-9
S1396 Resveratrol Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
Biochem Biophys Res Commun, 2024, 723:150186
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
S7046 Brefeldin A (BFA) Brefeldin A (BFA) is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR. Brefeldin A is also an inhibitor of autophagy and mitophagy.
Nat Commun, 2024, 15(1):203
Cancer Commun (Lond), 2024, 10.1002/cac2.12583
Cell Rep Med, 2024, S2666-3791(24)00544-5
S2285 Cryptotanshinone (Tanshinone C) Cryptotanshinone (Tanshinone C) is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
Bone Joint Res, 2024, 13(4):137-148
J Med Virol, 2023, 95(11):e29230
Microbiol Spectr, 2023, e0493222.
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Nat Commun, 2024, 15(1):7675
Microorganisms, 2024, 12(2)296
Autophagy, 2023, 19(11):2912-2933
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Cancer Discov, 2023, 13(3):598-615
Nat Commun, 2023, 14(1):2829
Cancer Res Commun, 2023, 3(4):659-671
S1792 Simvastatin Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.
J Immunother Cancer, 2024, 12(11)e009805
Cancer Med, 2024, 13(12):e7393
Neuron, 2023, S0896-6273(23)00513-5
S2556 Rosiglitazone Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Nat Commun, 2024, 15(1):1429
Nat Commun, 2024, 15(1):7991
Research (Wash D C), 2024, 7:0400
S1080 SU11274 SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.
Cancer Cell Int, 2024, 24(1):43
J Transl Med, 2023, 21(1):530
J Transl Med, 2023, 21(1):530
S2799 Daporinad (FK866) Daporinad (FK866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.
Cell Discov, 2024, 10(1):39
Theranostics, 2024, 14(7):2794-2815
Theranostics, 2024, 14(15):5999-6015
S1035 Pazopanib HCl Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.
iScience, 2023, 26(7):107116
NPJ Breast Cancer, 2022, 8(1):44
J Pers Med, 2022, 12(2)258
S2679 Flavopiridol (Alvocidib) HCl Flavopiridol (Alvocidib) HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.
Elife, 2024, 13e80684
Int J Biol Macromol, 2023, 258(Pt 1):128776
Mol Cell Biol, 2023, 43(1):1-21
S2658 Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1.
Mol Cancer, 2024, 23(1):78
Mol Cancer, 2024, 23(1):78
JCI Insight, 2024, 9(10)e164191
S1238 Tamoxifen Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
Nat Commun, 2024, 15(1):2377
Breast Cancer Res, 2024, 26(1):33
Toxics, 2024, 12(4)247
S1314 Zoledronic acid (Zoledronate) Zoledronic acid (Zoledronate), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
Cells, 2024, 13(10)862
Cells, 2024, 13(10)862
Cancer Immunol Immunother, 2024, 73(4):62
S2843 BI-D1870 BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.
Cells, 2024, 13(18)1546
Sci Rep, 2024, 14(1):9440
BMC Cancer, 2024, 24(1):233
S2163 PF-4708671 PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. PF-4708671 induces autophagy. First S6K1-specific inhibitor to be reported.
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
Int J Mol Sci, 2024, 25(7)3944
Am J Cancer Res, 2024, 14(3):1087-1100
S7164 GSK343 GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy.
Cancers (Basel), 2024, 16(9)1639
Sci Adv, 2024, 10(13):eadk4423
J Immunother Cancer, 2023, 11(11)e007736
S7130 PR-619 PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM in a cell-free assay. PR-619 activates autophagy.
Nat Commun, 2024, 15(1):1642
Mol Cell, 2024, 84(16):3115-3127.e11
BMC Biol, 2024, 22(1):71
S8047 Dynasore Dynasore is a cell-permeable, reversible non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2, with IC50 of 15 μM in a cell-free assay, also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase. Dynasore suppresses mTORC1 activity and induces autophagy. Dynasore inhibits the entry of several viruses, including herpes simplex virus (HSV).
Immunity, 2024, 57(2):287-302.e12
Nat Commun, 2024, 15(1):1669
Redox Biol, 2024, 76:103335
S7842 LY3009120 LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.
Drug Resist Updat, 2023, 71:100993
Exp Cell Res, 2023, 430(1):113722
Curr Issues Mol Biol, 2023, 45(7):5865-5878
S1190 Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
iScience, 2024, 27(3):109246
Cancers (Basel), 2024, 16(7)1303
Cancers (Basel), 2024, 16(2)296
S2061 Lovastatin Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM in a cell-free assay, used for lowering cholesterol (hypolipidemic agent). Lovastatin triggers autophagy.
Cell Discov, 2024, 10(1):39
Nat Commun, 2024, 15(1):6740
Int J Biol Sci, 2024, 20(6):2130-2148
S1590 TWS119 TWS119 is a GSK-3β inhibitor with IC50 of 30 nM in a cell-free assay; capable of inducing neuronal differentiation and may be useful to stem cell biology. GSK-3β inhibition triggers autophagy.
Nat Commun, 2024, 15(1):2089
Sci Rep, 2024, 14(1):5038
SLAS Discov, 2024, 29(8):100191
S1228 Idarubicin HCl Idarubicin HCl (4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy.
Cell Rep, 2024, 43(7):114388
BMC Pharmacol Toxicol, 2024, 25(1):25
Mol Cell, 2023, 83(13):2206-2221.e11
S3042 Purmorphamine Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.
Nat Commun, 2024, 15(1):987
J Adv Res, 2024, S2090-1232(24)00106-1
Neural Regen Res, 2024, 19(1):205-211
S1231 Topotecan HCl Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.
Mol Cell, 2024, 84(14):2618-2633.e10
Cancer Cell Int, 2024, 24(1):285
iScience, 2024, 27(1):108667
S7423 KN-93 Phosphate KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy.This product is not soluble in saline. Please do not dissolve it in saline for administration.
Eye Vis (Lond), 2024, 11(1):37
PLoS Pathog, 2023, 19(3):e1011295
Ren Fail, 2023, 45(1):2172961
S2219 Momelotinib (CYT387) Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
Cell Rep, 2023, 42(9):113067
Breast Cancer Res, 2023, 25(1):51
S7998 Entrectinib Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
Signal Transduct Target Ther, 2024, 9(1):153
Biomed Pharmacother, 2024, 176:116766
J Pathol, 2024, 263(2):257-269
S3030 Niclosamide Niclosamide can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5).
PLoS Pathog, 2024, 20(7):e1012352
Int J Nanomedicine, 2023, 18:7505-7521
Front Cell Dev Biol, 2023, 11:1062229
S7455 Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.
Cancer Cell, 2024, S1535-6108(24)00119-3
Nat Commun, 2024, 15(1):7662
Redox Biol, 2024, 70:103072
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Elife, 2024, 12RP92324
Sci Rep, 2024, 14(1):4303
Environ Mol Mutagen, 2024, 10.1002/em.22604
S2198 SGI-1776 free base SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. SGI-1776 induces apoptosis and autophagy.
Cell Death Dis, 2024, 15(9):644
Mar Drugs, 2024, 22(10)444
Mol Cancer, 2023, 22(1):64
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Clin Cancer Res, 2023, 29(2):446-457
Clin Cancer Res, 2023, 29(2):446-457
Cancer Cell Int, 2023, 23(1):207
S8006 BIX 01294 BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.
Acta Pharm Sin B, 2024, 14(3):1187-1203
Cell Commun Signal, 2024, 22(1):402
Dev Cell, 2023, 58(6):506-521.e5
S1135 Pemetrexed disodium Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
Cell Death Dis, 2024, 15(8):555
Cell Commun Signal, 2024, 22(1):375
Cancer Cell, 2022, 40(10):1128-1144.e8
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Cancer Cell Int, 2024, 24(1):303
Front Pharmacol, 2024, 15:1418902
PLoS Negl Trop Dis, 2024, 18(8):e0012428
S7033 GSK2656157 GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases. GSK2656157 decreases apoptosis and inhibits excessive autophagy.
Cancer Gene Ther, 2024, 10.1038/s41417-024-00818-z
Int J Mol Sci, 2024, 25(5)2611
Respir Res, 2024, 25(1):201
S7483 DMOG DMOG (Dimethyloxalylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy.Solutions are unstable and should be fresh-prepared.
Life Sci Alliance, 2025, 8(1)e202403053
Nat Cell Biol, 2024, 10.1038/s41556-024-01475-y
Immunology, 2024, 10.1111/imm.13797
S7751 VER155008 VER155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
Nat Cell Biol, 2024, 26(11):1943-1957
Breast Cancer Res, 2024, 26(1):33
Vet Res, 2024, 55(1):63
S7146 DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. DMH1 inhibits autophagy.
Nat Commun, 2024, 15(1):5817
J Exp Med, 2024, 221(5)e20221190
EMBO Rep, 2024, 25(3):1106-1129
S1896 Hydroxyurea Hydroxyurea is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.
Nature, 2024, 635(8037):201-209
Nat Commun, 2024, 15(1):7360
iScience, 2024, 27(4):109580
S7888 Spautin-1 Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. Spautin-1 enhances apoptosis.
Nat Commun, 2024, 15(1):9463
J Adv Res, 2024, S2090-1232(24)00025-0
Cancer Lett, 2024, 604:217258
S2624 OSI-027 OSI-027 (ASP4786, CERC 006, AEVI-006) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. OSI-027 induces autophagy in cancer cells.
J Cell Commun Signal, 2023, 17(3):975-989
Emerg Microbes Infect, 2022, 11(1):519-531
Mol Carcinog, 2022, 10.1002/mc.23414
S2476 Itraconazole Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Cell Infect Microbiol, 2023, 13:1131641
Front Cell Infect Microbiol, 2022, 12:864912
S2391 Quercetin Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
Cell Metab, 2024, S1550-4131(24)00371-1
Nucleic Acids Res, 2024, gkae322
Clin Transl Med, 2024, 14(5):e1660
S4505 Vinblastine sulfate Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.
Int J Mol Sci, 2024, 25(21)11346
PLoS One, 2024, 19(11):e0307153
Nat Commun, 2023, 14(1):7576
S4269 Vinorelbine ditartrate Vinorelbine ditartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin. Vinorelbine Tartrate exhibits anti-tumor activities via inducing the mitotic apoptosis, autophagy and inflammation.
Cell Death Dis, 2024, 15(8):603
BMC Pharmacol Toxicol, 2024, 25(1):25
BMC Pharmacol Toxicol, 2024, 25(1):25
S1235 Letrozole Letrozole is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM in cell-free assays.It has no effect on the plasma levels of 17α-OH progesterone, thyroid-stimulating hormone (TSH), luteinizing hormone (LH), follicle-stimulating hormone (FSH), or androstenedione and does not affect normal urine electrolyte excretion or thyroid function in clinical studies. Letrozole induces autophagy.
eNeuro, 2024, 11(8)ENEURO.0332-24.2024
J Chromatogr B Analyt Technol Biomed Life Sci, 2024, 1238:124106
Mol Oncol, 2023, 10.1002/1878-0261.13541
S2770 MK-5108 MK-5108 is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. MK-5108 (VX-689) induces autophagy. Phase 1.
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
Sci Rep, 2024, 14(1):4303
Biosensors (Basel), 2022, 12(4)196
S7104 AZD1208 AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.
Angiogenesis, 2024, 10.1007/s10456-024-09906-y
Cell Death Dis, 2024, 15(4):274
Inflamm Res, 2024, 10.1007/s00011-024-01924-2
S7949 MRT68921 HCl MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
Cell Death Differ, 2024, 10.1038/s41418-024-01260-2
J Exp Clin Cancer Res, 2024, 43(1):248
Cell Rep, 2024, 43(9):114728
S7885 SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.
Cell, 2024, 187(15):4043-4060.e30
Mol Cell, 2024, S1097-2765(24)00832-3
Cell Rep, 2024, 43(9):114728
S7785 Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. Pemetrexed Disodium Hydrate stimulates autophagy and apoptosis.
Cell Rep, 2022, 38(9):110448
Front Pharmacol, 2022, 13:1032975
J Pers Med, 2022, 12(2)258
S8222 AS1842856 AS1842856 is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 with IC50 of 33 nM. It could directly bind to the active Foxo1, but not the Ser256-phosphorylated form. AS1842856 suppresses autophagy.
Transl Res, 2024, S1931-5244(24)00051-3
CNS Neurosci Ther, 2024, 30(8):e14913
Cancer Res Commun, 2024, 4(5):1189-1198
S2713 Geldanamycin Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.
Nat Commun, 2024, 15(1):9448
Cell Rep, 2024, 43(10):114827
Int J Mol Sci, 2023, 24(18)13830
S1003 Linifanib (ABT-869) Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.
Cell Death Discov, 2023, 9(1):57
Cell Death Discov, 2023, 9(1):57
Cancer Cell, 2022, S1535-6108(22)00312-9
S1168 Valproic Acid sodium Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
J Exp Clin Cancer Res, 2024, 43(1):152
J Immunother Cancer, 2024, 12(11)e009805
Sci Total Environ, 2022, 838(Pt 2):155825
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
Mol Oncol, 2024, 10.1002/1878-0261.13577
Cell Metab, 2022, S1550-4131-2200411-9
S2635 CCT128930 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of CCT128930 triggers cell apoptosis in HepG2 cells.
Nat Commun, 2024, 15(1):6150
Cell Rep, 2024, 43(4):114108
Nat Commun, 2023, 14(1):886
S1204 Melatonin Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
Heliyon, 2024, 10(18):e38098
Heliyon, 2024, 10(11):e32571
Zhejiang Da Xue Xue Bao Yi Xue Ban, 2024, 53(4):498-508
S3944 VPA (Valproic acid) VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.
Sci Bull (Beijing), 2024, S2095-9273(24)00799-0
Nat Commun, 2024, 15(1):668
Dev Cell, 2024, S1534-5807(24)00326-5
S7682 SAR405 SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.
Cell, 2024, 187(15):4043-4060.e30
Nat Commun, 2024, 15(1):1277
Cancer Commun (Lond), 2024, 44(3):408-432
S2310 Honokiol Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Honokiol causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. Honokiol inhibits hepatitis C virus (HCV) infection. Phase 3.
Int J Nanomedicine, 2023, 18:4313-4327
Exp Gerontol, 2023, 173:112091
Cell Death Differ, 2022, 10.1038/s41418-022-01053-5
S4028 Dexamethasone Sodium Phosphate Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
Cancer Cell, 2024, 42(9):1507-1527.e11
Pharmaceutics, 2022, 14(2)400
Front Oncol, 2022, 12:888695
S8078 Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
Nat Commun, 2024, 15(1):7249
Sci Rep, 2024, 14(1):22572
Nat Commun, 2023, 14(1):3648
S7980 VPS34-IN1 Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy.
EMBO J, 2024, 10.1038/s44318-024-00096-3
bioRxiv, 2024, 10.1101/2024.01.22.575998
Nat Cell Biol, 2023, 25(7):975-988
S2782 GW4064 GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.
Gut Microbes, 2024, 16(1):2379566
Mol Metab, 2024, 79:101841
Chin Med, 2024, 19(1):16
S7381 Pepstatin A Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.
Cell Rep Med, 2024, 5(4):101503
Anim Nutr, 2024, 20:16:409-421.
Cells, 2024, 13(11)953
S2505 Rosiglitazone maleate Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
S1999 Sodium butyrate Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). Sodium butyrate (NaB) inhibits cell cycle progression, promotes differentiation, and induces apoptosis and autophagy in several types of cancer cells.
Nat Commun, 2024, 15(1):4764
Nat Commun, 2024, 15(1):5209
Cell Rep, 2024, 43(2):113778
S7165 UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. UNC1999 is a potent autophagy inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis.
Nat Commun, 2024, 15(1):7366
Acta Pharm Sin B, 2023, 13(6):2601-2612
Acta Pharm Sin B, 2023, 13(6):2601-2612
S7177 PF-543 hydrochloride PF-543 hydrochloride, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
J Transl Med, 2024, 22(1):43
Int J Mol Sci, 2023, 24(9)8303
Cell Res, 2022, 10.1038/s41422-022-00614-0
S7289 PFK15 PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.
Clin Exp Med, 2024, 24(1):219
Eur J Med Res, 2024, 29(1):236
Nat Commun, 2023, 14(1):5552
S2290 DHA (Dihydroartemisinin) DHA (Dihydroartemisinin) is a semi-synthetic derivative of artemisinin and isolated from the traditional Chinese herb Artemisia annua. Dihydroartemisinin induces autophagy and apoptosis by suppressing NF-κB activation.
Int Immunopharmacol, 2024, 139:112637
Front Pharmacol, 2024, 15:1418902
ACS Infect Dis, 2024, 10.1021/acsinfecdis.3c00588
S7680 SP2509 SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.
Nat Commun, 2024, 15(1):5631
bioRxiv, 2024, 2024.05.19.594897
MedComm (2020), 2023, 4(3):e269
S3022 Cabazitaxel Cabazitaxel is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.
J Photochem Photobiol B, 2024, 253:112877
Cancer Biol Ther, 2024, 25(1):2329368
Sci Adv, 2024, 10(5):eadg7887
S2606 Mifepristone Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Neuron, 2024, S0896-6273(24)00089-8
Cell Death Dis, 2024, 15(1):70
Cell Death Dis, 2024, 15(1):73
S3017 Aspirin Aspirin is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin induces autophagy and stimulates mitophagy.
Cell Death Discov, 2023, 10.1038/s41420-023-01664-y
iScience, 2023, 26(7):107105
Comput Struct Biotechnol J, 2022, 20:5750-5760
S5971 Pemetrexed Pemetrexed (LY231514) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
Cell Rep Med, 2024, 5(7):101615
Mol Cancer Res, 2024, 22(1):82-93
S1835 Azithromycin Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
Nat Commun, 2024, 15(1):6579
Int Immunopharmacol, 2024, 137:112426
mSphere, 2024, e0067124.
S2930 Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
Cell Mol Life Sci, 2024, 81(1):384
iScience, 2023, 26(7):107090
Heliyon, 2023, 9(3):e14169
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Cancer Cell, 2024, 42(4):535-551.e8
Sci Rep, 2024, 14(1):25682
Sci Rep, 2024, 14(1):879
S7215 Losmapimod Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.
Nat Commun, 2024, 15(1):987
Int J Mol Sci, 2024, 25(13)7302
J Radiat Res, 2024, rrae021
S1346 Heparin sodium Heparin sodium, a sulfated polysaccharide belonging to the family of glycosaminoglycans, has numerous important biological activities associated with its interaction with diverse proteins. Heparin is used as an anticoagulant primarily through its interaction with AT III by enhancing AT-IIImediated inhibition of blood coagulation factors, including thrombin and factor Xa. Heparin prevents the induction of autophagy.
Nat Commun, 2024, 15(1):9771
J Immunother Cancer, 2024, 12(11)e009805
Ecotoxicol Environ Saf, 2023, 252:114608
S1290 Celastrol Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.
Int J Biol Sci, 2024, 20(14):5731-5746
Int J Mol Sci, 2024, 25(10)5237
Fundam Res, 2024, 4(2):394-400
S5715 Atorvastatin Atorvastatin is a lipid lowering agent. It is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway. Atorvastatin activates autophagy.
MedComm (2020), 2024, 5(5):e525
Oncogene, 2024, 43(4):281-293
Mol Cancer, 2023, 22(1):147
S1759 Pitavastatin calcium Pitavastatin calcium, a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
Nat Commun, 2024, 15(1):4099
J Immunother Cancer, 2024, 12(11)e009805
Cell Rep, 2024, 43(6):114286
S1218 Clofarabine Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.
Front Oncol, 2023, 13:1287444
Cancer Res, 2022, 82(4):721-733
Clin Transl Med, 2022, 12(2):e747
S7134 IU1 IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μ M, 25-fold selective to IsoT. IU1 induces autophagy.
Redox Biol, 2024, 76:103318
Antioxidants (Basel), 2024, 13(1)114
Nat Commun, 2022, 13-1:5644
S7683 PIK-III PIK-III (VPS34-IN2), which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively.
Cell Rep, 2024, 43(1):113575
Sci Rep, 2024, 14(1):4000
Nucleic Acids Res, 2023, gkad342
S1972 Tamoxifen Citrate Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.
bioRxiv, 2024, 2023.05.10.540211
RNA, 2023, 29(9):1325-1338.
RNA, 2023, rna.079509.122
S1312 STZ (Streptozotocin) STZ (Streptozotocin) is a glucosamine-nitrosourea compound derived from Streptomyces achromogenes, which is a DNA-methylating, carcinogenic, antibiotic and diabetes inducing agent. Streptozotocin induces autophagy and apoptosis. Streptozotocin (STZ) can be used to induce animal models of diabetes. Solutions are unstable and should be fresh-prepared.
Cell Commun Signal, 2024, 22(1):368
Fluids Barriers CNS, 2024, 21(1):26
CNS Neurosci Ther, 2024, 30(8):e14913
S7724 Eprenetapopt (APR-246) Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.
Oncotarget, 2024, 15:614-633
J Cell Mol Med, 2024, 28(9):e18374
Cell Death Dis, 2023, 14(11):783
S7660 Obeticholic Acid (INT-747) Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.
iScience, 2024, 27(3):109118
Phytomedicine, 2023, 119:155005
Nat Commun, 2022, 13(1):3419
S2812 (R)-(-)-Gossypol (AT-101) acetic acid (R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.
Protein Cell, 2024, pwad065
Int J Mol Sci, 2023, 24(7)6662
Cancer Cell, 2022, S1535-6108(22)00312-9
S3031 Linagliptin (GSK2118436) Linagliptin (GSK2118436) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells.
Pharmacol Res, 2024, 207:107298
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
J Pers Med, 2022, 12(2)258
S1576 Sulfasalazine Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Med Oncol, 2024, 41(8):188
Adv Sci (Weinh), 2023, 10(20):e2300517
Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
S7793 Purvalanol A Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy.
Biomacromolecules, 2024, 10.1021/acs.biomac.4c00672
Cancers (Basel), 2023, 10.3390/cancers15225424
Cancer Res, 2022, canres.1707.2021
S2751 Milciclib Milciclib is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7, it's also an inhibitor of TRKA with IC50 of 53nM. Milciclib (PHA-848125) induces cell death through autophagy. Phase 2.
medRxiv, 2023, 2023.11.13.23298409
Nat Commun, 2022, 13(1):2725
ProQuest, 2022, 29166130
S1219 YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy.
Mol Biol Cell, 2024, 35(5):ar70
Nat Commun, 2022, 13(1):2136
Blood Cancer J, 2022, 12(3):39
S1351 Ivermectin Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
J Clin Invest, 2024, 134(22)e181314
Viruses, 2024, 16(4)640
Life Sci Alliance, 2023, 6(8)e202302133
S7067 Tepotinib Tepotinib is a potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib (EMD 1214063) induces autophagy. Phase 1.
Oncogene, 2024, 10.1038/s41388-024-02987-5
Int J Mol Sci, 2024, 25(3)1769
Int J Mol Sci, 2024, 25(3)1769
S7948 MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.
EMBO J, 2024, 10.1038/s44318-024-00244-9
mBio, 2023, 10.1128/mbio.02506-23
Viruses, 2023, 15(5)1112
S1847 Clemastine fumarate Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Glia, 2024, 72(9):1555-1571
Neurobiol Dis, 2024, 190:106375
J Clin Invest, 2022, e152187
S1794 Fenofibrate Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.
J Immunother Cancer, 2024, 12(11)e009805
Heliyon, 2024, 10(11):e31861
Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
S7343 URMC-099 URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
Cell Commun Signal, 2023, 21(1):82
Oncogene, 2023, 42(14):1132-1143.
Oncogenesis, 2023, 12(1):35
S8274 STO-609 STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy.
Acta Pharm Sin B, 2024, 14(8):3576-3590
J Transl Med, 2024, 22(1):844
PLoS One, 2024, 19(9):e0309794
S8808 DC661 DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than HCQ. DC661 induces apoptosis.
Autophagy, 2024, 1-13.
J Clin Invest, 2023, 133(8)e164596
J Clin Invest, 2023, 133(8)e164596
S3592 4-PBA (4-Phenylbutyric acid) 4-PBA (4-Phenylbutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models.
Int J Biol Sci, 2024, 20(4):1279-1296
Phytomedicine, 2024, 135:156088
J Transl Med, 2024, 22(1):248
S1403 Tigecycline Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline induces autophagy by downregulating the PI3K-AKT-mTOR pathway.
Int J Mol Sci, 2024, 25(9)4887
Int J Mol Sci, 2024, 25(9)4887
Antimicrob Agents Chemother, 2024, 68(3):e0112023
S1627 Nitazoxanide Nitazoxanide is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent(IC50 for canine influenza virus ranges from 0.17 to 0.21 μM). Nitazoxanide modulates autophagy and inhibits mTORC1 signaling.
Nat Commun, 2024, 15(1):8708
Mol Ther, 2024, S1525-0016(24)00340-X
Biomed Pharmacother, 2024, 171:116195
S1979 Amiodarone HCl Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.
J Immunother Cancer, 2024, 12(11)e009805
Cell Rep Methods, 2023, 3(4):100440
Cell Rep Methods, 2023, 3(4):100440
S4895 Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Nat Commun, 2024, 15(1):2089
J Pharm Sci, 2022, 111(8):2180-2190
EMBO Mol Med, 2021, e11814
S8793 ULK-101 ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively.
Immunity, 2024, 57(2):287-302.e12
Cell Rep, 2024, 43(1):113575
Sci Rep, 2024, 14(1):4000
S2077 Atorvastatin Calcium Atorvastatin Calcium is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol. Atorvastatin Calcium induces apoptosis and autophagy.
J Immunother Cancer, 2024, 12(11)e009805
Cancers (Basel), 2022, 14(9)2327
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
S7684 Salirasib Salirasib (Farnesylthiosalicylic acid, FTS) is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Phase 2.
J Biol Chem, 2023, 299(4):103017
Microbiol Spectr, 2023, 11(4):e0055223
Nat Commun, 2022, 13(1):7113
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. 3BDO inhibits oxLDL-induced apoptosis.
NPJ Parkinsons Dis, 2024, 10(1):52
Adv Sci (Weinh), 2023, 10(13):e2205436
Research Square, 2023, 10.21203/rs.3.rs-3629594/v1
S4211 Montelukast Sodium Montelukast Sodium selectively antagonizes leukotriene D4 (LTD4) by binding to it so that block the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1. Montelukast improves macroautophagy but not the chaperone-mediated autophagy pathway. Solutions are unstable and should be fresh-prepared.
Biochem Biophys Res Commun, 2022, 594:31-37
Cancer Immunol Immunother, 2021, 70(1):203-213
Aging (Albany NY), 2021, 13(24):25670-25693
S8369 Lys05 Lys05 is a new lysosomal autophagy inhibitor which potently accumulates within and deacidifies the lysosome of both cells and tumors, resulting in sustained inhibition of autophagy and tumor growth.
Immunity, 2024, 57(11):2651-2668.e12
Sci Rep, 2024, 14(1):4000
Nat Cell Biol, 2022, 24(8):1202-1210
S2480 Loperamide HCl Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease.
Front Neurosci, 2024, 18:1424936
Front Cell Infect Microbiol, 2023, 13:1139152
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
S8596 Autophinib Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.
Cancer Commun (Lond), 2024, 44(3):408-432
Cancer Commun (Lond), 2024, 44(3):408-432
Burns Trauma, 2024, 12:tkad057
S8807 PFK158 PFK158 is a potent and selective inhibitor of PFKFB3. It has improved PK properties and causes ~80% growth inhibition in several mouse models of human-derived tumors.
Nat Metab, 2022, 4(10):1287-1305
Cancers (Basel), 2022, 14(9)2113
Front Oncol, 2022, 12:826655
S1389 Omeprazole Omeprazole is a proton pump inhibitor that blocks H(+)-K(+)-ATPase, used to treat dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome.
J Extracell Vesicles, 2024, 13(4):e12426
J Extracell Vesicles, 2024, 13(4):e12426
J Transl Med, 2024, 22(1):676
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy.
Sci Rep, 2024, 14(1):8200
bioRxiv, 2023, 10.1101/2023.12.19.572304
Burns Trauma, 2020, 8:tkaa025
S4484 Trametinib DMSO solvate Trametinib DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis.
JID Innov, 2024, 4(2):100248
Cell Rep, 2022, 38(7):110374
Mol Cell Proteomics, 2022, 21(6):100240
S2181 Ixazomib Citrate (MLN9708) Analogue Ixazomib Citrate (MLN9708) Analogue is the analogue of Ixazomib Citrate (MLN9708) from WO2016165677A1. Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Ixazomib (MLN2238) induces autophagy. Phase 3.
EMBO J, 2023, 42(17):e111719
iScience, 2023, 26(6):106997
J Dermatol Sci, 2022, S0923-1811(22)00125-6
S1693 Carbamazepine Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
J Immunother Cancer, 2024, 12(11)e009805
mBio, 2022, e0217721
Front Pharmacol, 2021, 12:749930
S7648 OTS964 OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts.
Nucleic Acids Res, 2023, gkad001
Cancer Lett, 2022, 544:215812
Cell Death Dis, 2022, 13(5):450
S8240 SMER28 SMER28 is a small-molecule enhancer (SMER) of autophagy, inducing autophagy independently of rapamycin in mammalian cells.
Nat Chem Biol, 2020, 6
Cell Rep, 2020, 31(12):107800
Cell Rep, 2019, 27(12):3413-3421
S5144 Neferine Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.
Bone Res, 2022, 10(1):27
Cell Death Dis, 2022, 13(11):1000
iScience, 2022, 25(11):105394
S1733 Methylprednisolone Methylprednisolone is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
Food Chem Toxicol, 2024, 188:114665
Drug Test Anal, 2020, 10.1002/dta.2917
Nat Med, 2017, 23(4):424-428
S1747 Nimodipine Nimodipine (BAY E 9736) is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.
J Immunother Cancer, 2024, 12(11)e009805
Eye Vis (Lond), 2024, 11(1):37
Cell Discov, 2020, 6(1):96
S8597 LYN-1604 LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
J Virol, 2021, JVI0155021
Exp Eye Res, 2019, 184:126-134
S6912 Vacuolin-1 Vacuolin-1 is a potent and cell-permeable inhibitor that blocks the Ca(2+)-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. Vacuolin-1 is also a potent and selective PIKfyve inhibitor, and inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition.
Virulence, 2024, 15(1):2350893
Virulence, 2024, 15(1):2350893
Nat Commun, 2023, 14(1):3997
S3653 Spermidine trihydrochloride Spermidine (4-Azaoctamethylenediamine), a natural polyamine produced from putrescine and decarboxylated S-adenosylmethionine (dcSAM) by spermidine synthase, is a novel autophagy inducer and negatively modulates N-methyl-d-aspartate (NMDA).
Cell Metab, 2023, S1550-4131(23)00341-8
Int J Mol Sci, 2021, 22(19)10255
Int J Mol Sci, 2021, 22(19), 10255
S3758 Sinomenine hydrochloride Sinomenine (SN, Cucoline, Kukoline, Sabianine A), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent.
Biomed Res Int, 2022, 2022:4914005
Cancer Manag Res, 2021, 13:1189-1204
Bioorg Med Chem, 2020, 31:115986
S8432 Troglitazone Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
CNS Neurosci Ther, 2024, 30(8):e14911
Int J Mol Med, 2024, 53(4)37
Free Radic Biol Med, 2021, 163:234-242
S1837 Flubendazole Flubendazole (Flumoxanal, NSC 313680) is an autophagy inducer by targeting Atg4B, used to treat internal parasite and worm infection.
Nat Commun, 2024, 15(1):4513
Sci Rep, 2020, 10(1):13124
RSC Advances, 2018, 10.1039/C7RA12259D
S0709 Tubastatin A TFA Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
Cell Mol Life Sci, 2023, 80(11):333
Cell Mol Life Sci, 2023, 80(11):333
Drug Dev Res, 2022, 10.1002/ddr.21927
S8576 EAD1 EAD1 is a potent autophagy inhibitor with an IC50 of 5.8 μM in the BxPC3 cells. It has antiproliferative activities in lung and pancreatic cancer cells.
Mol Cancer Ther, 2022, 21(1):79-88
Autophagy, 2021, 1-17
S6650 EN6 EN6 is a novel covalent autophagy activator and targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase with an IC50 of 1.7 μM for recombinant human ATP6V1A protein.
Cell Death Dis, 2021, 12(1):119
Life (Basel), 2021, 11(9)948
Brain Res, 2021, 1778:147768
S8527 ROC-325 ROC-325 is an orally available novel inhibitor of lysosomal-mediated autophagy which diminishes AML cell viability with the IC50 range of 0.7-2.2 μM.
Front Pharmacol, 2024, 15:1344075
Elife, 2023, 12e83205
Adv Sci (Weinh), 2022, 9(27):e2105938
S6847 ML-9 HCl ML-9 HCl (ML-9 hydrochloride) is a selective and potent inhibitor of Akt kinase, myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). ML-9 HCl is also a potent inhibitor of Ca2+-permeable channels. ML-9 HCl is a lysosomotropic agent targeting autophagy and cell death.
PLoS Pathog, 2023, 19(3):e1011295
J Mol Endocrinol, 2019, 63(3):199-213
S6889 Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
Cell Cycle, 2022, 1-11.
Aging (Albany NY), 2021, 13(13):17097-17117
S6716 NSC 185058 NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways.
STAR Protoc, 2024, 5(3):103181
Biochem Biophys Res Commun, 2022, 632:40-47
Sci Adv, 2022, 8(31):eabo0412
S6301 MPP+ iodide MPP+ iodide (N-Methyl-4-Phenylpyridinium Iodide), the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces autophagic cell death in SH-SY5Y cells. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA) neurons, but internalization of serotonin transporter (SERT) in serotonergic (5-HT) neurons.
Front Immunol, 2023, 14:1193081
Front Immunol, 2023, 14:1193081
S1041 STF-62247 STF-62247 is a molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. STF-62247 shows selective toxicity and growth inhibition of renal cells lacking VHL; 25-fold greater sensitivity observed for cells with VHL deficiency compared to wild-type (VHL+).
Neuropsychiatr Dis Treat, 2015, 11:2091-9
S2458 Clonidine HCl Clonidine HCl(Kapvay) is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg.
J Immunother Cancer, 2024, 12(11)e009805
Mol Pain, 2022, 18:17448069221107810
S8764 IITZ-01 IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function.
Cancers (Basel), 2020, 12(9):E2363
S8943 VLX600 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity.
Cancers (Basel), 2022, 14(13)3225
S3698 Nortriptyline hydrochloride Nortriptyline hydrochloride (Desitriptyline, ELF-101, EN-7048, Desmethylamitriptyline) is the hydrochloride salt form of nortriptyline, a tricyclic antidepressant agent used for short-term treatment of various forms of depression.
Front Bioinform, 2021, 1:710591
S6797 QX77 QX77 is a novel activator of chaperone-mediated autophagy (CMA). QX77 induces the up-regulation of Rab11 expression and up-regulates LAMP2A expression.
Autophagy, 2024, 10.1080/15548627.2024.2395797
Front Pharmacol, 2021, 12:707259
S6919 Brevilin A Brevilin A (6-O-Angeloylplenolina), a sesquiterpene lactone isolated from Centipeda minima, is a selective inhibitor of STAT3 and attenuates the JAKs activity by blocking the JAKs tyrosine kinase domain JH1. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.
Front Pharmacol, 2022, 13:795613
S4081 Sulfacetamide Sodium Sulfacetamide Sodium is an anti-biotic.
G3 (Bethesda), 2020, 4;10(5):1585-1597
S5920 CA-5f CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
J Virol, 2021, JVI0155021
S6078 ICCB-19 hydrochloride ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy.
Cell Death Discov, 2023, 9(1):109
S6471 Lucanthone Lucanthone is a novel autophagic inhibitor and also an orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1.
Int J Mol Sci, 2021, 23(1)17
S6395 CA77.1 CA77.1 (CA) is a potent, brain-penetrant and orally active activator of chaperone-mediated autophagy (CMA) for the treament of Alzheimer's disease (AD).
Sci Adv, 2023, 9(40):eadi8343
S9150 Daurisoline Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects.
Biochem Pharmacol, 2024, 223:116113
Cell Death Dis, 2022, 13(11):1000
S2491 Nitrendipine Nitrendipine (Bayotensin) is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.
Nat Commun, 2024, 15(1):8708
S4643 KB-R7943 mesylate KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. KB-R7943 mesylate promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux.
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis.
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
E4824New Hydroxychloroquine Hydroxychloroquine (HCQ) is an antimalarial drug that inhibits autophagy and is used to treat systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA). It exhibits immunomodulatory, antithrombotic, and antiplatelet properties. It inhibits the release endothelin-1, a potent vasoconstrictor, and restores impaired angiogenesis in TNF-α-treated endothelial cells in vitro. It also reduces the production of inflammatory cytokines such as TNF-α, IFN-γ, and IL-6 from peripheral blood mononuclear cells, upregulates IL-10 and decreases platelet aggregation.
Cancer Lett, 2024, 596:217009
Int J Mol Sci, 2022, 23(22)14149
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
S1027 FL-411 FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction.
S5973 Methylprednisolone Acetate Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
E4809New Piperaquine tetraphosphate tetrahydrate Piperaquine tetraphosphate tetrahydrate is an inhibitor of autophagy . It is a bisquinoline antimalarial agent effective against Plasmodium falciparum. Piperaquine tetraphosphate tetrahydrate is useful in antimalarial research.
S8964 Actinomycin D (Dactinomycin) Actinomycin D (Dactinomycin, Act D, RASP-101) is a significant polypeptide antibiotic isolated from soil bacteria of the genus Streptomyces. Actinomycin D (Dactinomycin) inhibits DNA repair and rests the cell cycle at G1 phase with IC50 of 0.42 μM and 0.4 nM, respectively. Actinomycin D is an autophagy activator, induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
Mol Cancer, 2024, 23(1):186
Nat Commun, 2024, 15(1):5209
Exp Mol Med, 2024, 10.1038/s12276-024-01315-x
S6957 β-Elemene

β-Elemene ((-)-β-Elemene, Levo-β-elemene) is a sesquiterpene compound extracted from the herb Curcuma Rhizoma with antitumor activities. β-elemene can inhibit cell proliferation, arrest the cell cycle, and induce cell apoptosis or autophagy.

S4750 Sulfacetamide sodium salt hydrate Sulfacetamide is a sulfonamide antibiotic that blocks the synthesis of dihydrofolic acid by inhibiting the enzyme dihydropteroate synthase(DHPS) with IC50 of 9.5 μM. Sulfacetamide is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), which is required for bacterial synthesis of folic acid.
S9027 Corynoxine Corynoxine, a natural oxindole alkaloid, is a new autophagy enhancer.
E3586 Myristica fragrans Extract Myristica Fragrans Extract is extracted from Myristica Fragrans, which has autophagy modulating activity.
S8744 PHY34 PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
S9860 BC1618 BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.
S9424 Liensinine diperchlorate Liensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor.
E3141 Codonopsis Pilosula Extract Codonopsis Pilosula Extract is obtained from Codonopsis pilosula, exhibits not only an anti-melanogenic effect in normal melanocytes, but also a cytoprotective effect in melanocytes subjected to oxidative stress by inducing autophagy and microphthalmia-associated transcription factor (MITF) expression.
S9611 ABTL-0812 ABTL0812 (α-Hydroxylinoleic acid, LP-10218, SCLN-0812) inhibits Akt/mTOR axis by inducing the overexpression of TRIB3 and activating autophagy in lung squamous carcinoma cell lines. ABTL0812 also induces AMPK activation and ROS accumulation.
S3890 Leonurine Leonurine, an active alkaloid extracted from Traditional Chinese Medicine Herba leonuri, exerts several biological effects, such as antidiabetic, cardiovascular, and bovine mastitis protection.
Chem Biol Interact, 2024, 395:111016
S4476 PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells.
S6851 RA-190 RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.
S3569 Spermidine Spermidine is a natural polyamine that stimulates cytoprotective macroautophagy/autophagy.
Cell Metab, 2023, S1550-4131(23)00341-8
Oxid Med Cell Longev, 2022, 2022:8033353
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
S4546 Xylitol Xylitol (Adonitol, Ribitol, Xylite, D-Xylitol, Adonite) is a sugar alcohol derived from XYLOSE by reduction of the carbonyl group. It is as sweet as sucrose and used as a noncariogenic sweetener.
S0012 E260 E260 (Fer and FerT inhibitor E260) is a Fer kinase and FerT inhibitor that selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level.
S9310 Isorhychophylline Isorhynchophylline (IsoRhy, 7-Isorhyncophylline) is a major tetracyclic oxindole alkaloid isolated from the Chinese herbal medicine Uncaria rhynchophylla (Miq.)Jacks (Gouteng in Chinese). It acts as a neuronal autophagy inducer with therapeutic potential for cardiovascular and central nervous system diseases.
E4692New THZ-P1-2 THZ-P1-2 is an inhibitor of PI5P4K, which covalently binds to cysteines on a disordered loop in PI5P4Kα/β/γ. It inhibits PI5P4Kα kinase activity with an IC50 of 190 nM and disrupts autophagy by impairing autophagosome clearance and increasing TFEB nuclear localization.
E1232 Concanavalin A Concanavalin A is a potential anti-neoplastic agent targeting apoptosis, autophagy and anti-angiogenesis for cancer therapeutics.
S1105 LY294002 LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Signal Transduct Target Ther, 2024, 9(1):109
Signal Transduct Target Ther, 2024, 9(1):109
Nat Genet, 2024, 10.1038/s41588-024-01891-8
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Cancer Cell, 2024, 42(4):535-551.e8
Nat Commun, 2024, 15(1):2581
Nat Commun, 2024, 15(1):987
S1013 Bortezomib Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.
Cell, 2024, 187(18):4905-4925.e24
Cell, 2024, S0092-8674(24)00315-5
Cell, 2024, S0092-8674(24)00653-6
S2767 3-MA (3-Methyladenine) 3-MA (3-Methyladenine) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. Solutions are unstable and should be fresh-prepared.
Bioact Mater, 2024, 32:277-291
Nat Commun, 2024, 15(1):1669
Adv Sci (Weinh), 2024, 11(32):e2400952
S1102 U0126-EtOH U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.
MedComm (2020), 2024, 5(5):e525
Int J Biol Sci, 2024, 20(6):2202-2218
Cell Death Dis, 2024, 15(1):31
S1150 Paclitaxel Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy.
Bioact Mater, 2025, 43:67-81
Nat Commun, 2024, 15(1):2503
Nat Commun, 2024, 15(1):2089
S1413 Bafilomycin A1 (Baf-A1) Bafilomycin A1(Baf-A1) is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.
Nature, 2024, 626(8000):874-880
Nature, 2024, 626(8000):874-880
Cell, 2024, 187(21):6055-6070.e22
S1092 KU-55933 KU-55933 is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
Nature, 2024, 629(8011):443-449
Nature, 2024, 629(8011):443-449
Cell, 2024, 187(20):5698-5718.e26
S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nature, 2024, 10.1038/s41586-024-07990-0
Nat Commun, 2024, 15(1):451
Nat Commun, 2024, 15(1):4926
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Leukemia, 2024, 38(5):969-980
Clin Transl Med, 2024, 14(5):e1703
Clin Transl Med, 2024, 14(5):e1703
S8037 Necrostatin-1 Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
Mol Cancer, 2024, 23(1):113
Mil Med Res, 2024, 11(1):22
Redox Biol, 2024, 75:103270
S1490 Ponatinib Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
Int J Biol Sci, 2024, 20(9):3412-3425
Cell Rep, 2024, 43(3):113932
Elife, 2024, 12RP92324
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Nat Commun, 2024, 15(1):1642
Cancer Lett, 2024, 604:217258
Phytomedicine, 2024, 135:156053
S1786 Verteporfin Verteporfin is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis.
Acta Pharm Sin B, 2024, 14(3):1222-1240
Bone Res, 2024, 12(1):12
Cancer Lett, 2024, 587:216692
S6999 Chloroquine Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Signal Transduct Target Ther, 2024, 9(1):65
Mol Cancer, 2024, 23(1):240
Bioact Mater, 2024, 32:277-291
S2704 LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocks autophagy and induces apoptosis.
Cell Mol Life Sci, 2024, 81(1):173
Cell Mol Life Sci, 2024, 81(1):173
Int J Mol Sci, 2024, 25(2)959
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
EMBO J, 2024, 10.1038/s44318-024-00244-9
EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9
CNS Neurosci Ther, 2024, 30(8):e14913
S2775 Nocodazole Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
Nat Commun, 2024, 15(1):9771
Nucleic Acids Res, 2024, gkae605
S4430 Hydroxychloroquine (HCQ) Sulfate Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Redox Biol, 2024, 75:103274
Phytomedicine, 2024, 10.1016/j.phymed.2023.155152
Breast Cancer Res, 2024, 26(1):33
S7811 MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
Bone Res, 2024, 12(1):15
J Exp Clin Cancer Res, 2024, 43(1):112
Sci Total Environ, 2024, 921:171101
S7046 Brefeldin A (BFA) Brefeldin A (BFA) is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR. Brefeldin A is also an inhibitor of autophagy and mitophagy.
Nat Commun, 2024, 15(1):203
Cancer Commun (Lond), 2024, 10.1002/cac2.12583
Cell Rep Med, 2024, S2666-3791(24)00544-5
S3042 Purmorphamine Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.
Nat Commun, 2024, 15(1):987
J Adv Res, 2024, S2090-1232(24)00106-1
Neural Regen Res, 2024, 19(1):205-211
S7423 KN-93 Phosphate KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy.This product is not soluble in saline. Please do not dissolve it in saline for administration.
Eye Vis (Lond), 2024, 11(1):37
PLoS Pathog, 2023, 19(3):e1011295
Ren Fail, 2023, 45(1):2172961
S7455 Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.
Cancer Cell, 2024, S1535-6108(24)00119-3
Nat Commun, 2024, 15(1):7662
Redox Biol, 2024, 70:103072
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Clin Cancer Res, 2023, 29(2):446-457
Clin Cancer Res, 2023, 29(2):446-457
Cancer Cell Int, 2023, 23(1):207
S7033 GSK2656157 GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases. GSK2656157 decreases apoptosis and inhibits excessive autophagy.
Cancer Gene Ther, 2024, 10.1038/s41417-024-00818-z
Int J Mol Sci, 2024, 25(5)2611
Respir Res, 2024, 25(1):201
S7751 VER155008 VER155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
Nat Cell Biol, 2024, 26(11):1943-1957
Breast Cancer Res, 2024, 26(1):33
Vet Res, 2024, 55(1):63
S7146 DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. DMH1 inhibits autophagy.
Nat Commun, 2024, 15(1):5817
J Exp Med, 2024, 221(5)e20221190
EMBO Rep, 2024, 25(3):1106-1129
S7888 Spautin-1 Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. Spautin-1 enhances apoptosis.
Nat Commun, 2024, 15(1):9463
J Adv Res, 2024, S2090-1232(24)00025-0
Cancer Lett, 2024, 604:217258
S7949 MRT68921 HCl MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
Cell Death Differ, 2024, 10.1038/s41418-024-01260-2
J Exp Clin Cancer Res, 2024, 43(1):248
Cell Rep, 2024, 43(9):114728
S7885 SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.
Cell, 2024, 187(15):4043-4060.e30
Mol Cell, 2024, S1097-2765(24)00832-3
Cell Rep, 2024, 43(9):114728
S8222 AS1842856 AS1842856 is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 with IC50 of 33 nM. It could directly bind to the active Foxo1, but not the Ser256-phosphorylated form. AS1842856 suppresses autophagy.
Transl Res, 2024, S1931-5244(24)00051-3
CNS Neurosci Ther, 2024, 30(8):e14913
Cancer Res Commun, 2024, 4(5):1189-1198
S7682 SAR405 SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.
Cell, 2024, 187(15):4043-4060.e30
Nat Commun, 2024, 15(1):1277
Cancer Commun (Lond), 2024, 44(3):408-432
S7381 Pepstatin A Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.
Cell Rep Med, 2024, 5(4):101503
Anim Nutr, 2024, 20:16:409-421.
Cells, 2024, 13(11)953
S7289 PFK15 PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.
Clin Exp Med, 2024, 24(1):219
Eur J Med Res, 2024, 29(1):236
Nat Commun, 2023, 14(1):5552
S1835 Azithromycin Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
Nat Commun, 2024, 15(1):6579
Int Immunopharmacol, 2024, 137:112426
mSphere, 2024, e0067124.
S2930 Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
Cell Mol Life Sci, 2024, 81(1):384
iScience, 2023, 26(7):107090
Heliyon, 2023, 9(3):e14169
S1346 Heparin sodium Heparin sodium, a sulfated polysaccharide belonging to the family of glycosaminoglycans, has numerous important biological activities associated with its interaction with diverse proteins. Heparin is used as an anticoagulant primarily through its interaction with AT III by enhancing AT-IIImediated inhibition of blood coagulation factors, including thrombin and factor Xa. Heparin prevents the induction of autophagy.
Nat Commun, 2024, 15(1):9771
J Immunother Cancer, 2024, 12(11)e009805
Ecotoxicol Environ Saf, 2023, 252:114608
S7683 PIK-III PIK-III (VPS34-IN2), which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively.
Cell Rep, 2024, 43(1):113575
Sci Rep, 2024, 14(1):4000
Nucleic Acids Res, 2023, gkad342
S7660 Obeticholic Acid (INT-747) Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.
iScience, 2024, 27(3):109118
Phytomedicine, 2023, 119:155005
Nat Commun, 2022, 13(1):3419
S7948 MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.
EMBO J, 2024, 10.1038/s44318-024-00244-9
mBio, 2023, 10.1128/mbio.02506-23
Viruses, 2023, 15(5)1112
S8274 STO-609 STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy.
Acta Pharm Sin B, 2024, 14(8):3576-3590
J Transl Med, 2024, 22(1):844
PLoS One, 2024, 19(9):e0309794
S8808 DC661 DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than HCQ. DC661 induces apoptosis.
Autophagy, 2024, 1-13.
J Clin Invest, 2023, 133(8)e164596
J Clin Invest, 2023, 133(8)e164596
S8793 ULK-101 ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively.
Immunity, 2024, 57(2):287-302.e12
Cell Rep, 2024, 43(1):113575
Sci Rep, 2024, 14(1):4000
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. 3BDO inhibits oxLDL-induced apoptosis.
NPJ Parkinsons Dis, 2024, 10(1):52
Adv Sci (Weinh), 2023, 10(13):e2205436
Research Square, 2023, 10.21203/rs.3.rs-3629594/v1
S8369 Lys05 Lys05 is a new lysosomal autophagy inhibitor which potently accumulates within and deacidifies the lysosome of both cells and tumors, resulting in sustained inhibition of autophagy and tumor growth.
Immunity, 2024, 57(11):2651-2668.e12
Sci Rep, 2024, 14(1):4000
Nat Cell Biol, 2022, 24(8):1202-1210
S8596 Autophinib Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.
Cancer Commun (Lond), 2024, 44(3):408-432
Cancer Commun (Lond), 2024, 44(3):408-432
Burns Trauma, 2024, 12:tkad057
S8807 PFK158 PFK158 is a potent and selective inhibitor of PFKFB3. It has improved PK properties and causes ~80% growth inhibition in several mouse models of human-derived tumors.
Nat Metab, 2022, 4(10):1287-1305
Cancers (Basel), 2022, 14(9)2113
Front Oncol, 2022, 12:826655
S1733 Methylprednisolone Methylprednisolone is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
Food Chem Toxicol, 2024, 188:114665
Drug Test Anal, 2020, 10.1002/dta.2917
Nat Med, 2017, 23(4):424-428
S6912 Vacuolin-1 Vacuolin-1 is a potent and cell-permeable inhibitor that blocks the Ca(2+)-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. Vacuolin-1 is also a potent and selective PIKfyve inhibitor, and inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition.
Virulence, 2024, 15(1):2350893
Virulence, 2024, 15(1):2350893
Nat Commun, 2023, 14(1):3997
S3758 Sinomenine hydrochloride Sinomenine (SN, Cucoline, Kukoline, Sabianine A), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent.
Biomed Res Int, 2022, 2022:4914005
Cancer Manag Res, 2021, 13:1189-1204
Bioorg Med Chem, 2020, 31:115986
S8576 EAD1 EAD1 is a potent autophagy inhibitor with an IC50 of 5.8 μM in the BxPC3 cells. It has antiproliferative activities in lung and pancreatic cancer cells.
Mol Cancer Ther, 2022, 21(1):79-88
Autophagy, 2021, 1-17
S8527 ROC-325 ROC-325 is an orally available novel inhibitor of lysosomal-mediated autophagy which diminishes AML cell viability with the IC50 range of 0.7-2.2 μM.
Front Pharmacol, 2024, 15:1344075
Elife, 2023, 12e83205
Adv Sci (Weinh), 2022, 9(27):e2105938
S6716 NSC 185058 NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways.
STAR Protoc, 2024, 5(3):103181
Biochem Biophys Res Commun, 2022, 632:40-47
Sci Adv, 2022, 8(31):eabo0412
S8764 IITZ-01 IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function.
Cancers (Basel), 2020, 12(9):E2363
S3698 Nortriptyline hydrochloride Nortriptyline hydrochloride (Desitriptyline, ELF-101, EN-7048, Desmethylamitriptyline) is the hydrochloride salt form of nortriptyline, a tricyclic antidepressant agent used for short-term treatment of various forms of depression.
Front Bioinform, 2021, 1:710591
S5920 CA-5f CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
J Virol, 2021, JVI0155021
S6471 Lucanthone Lucanthone is a novel autophagic inhibitor and also an orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1.
Int J Mol Sci, 2021, 23(1)17
S9150 Daurisoline Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects.
Biochem Pharmacol, 2024, 223:116113
Cell Death Dis, 2022, 13(11):1000
S4643 KB-R7943 mesylate KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. KB-R7943 mesylate promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux.
E4824New Hydroxychloroquine Hydroxychloroquine (HCQ) is an antimalarial drug that inhibits autophagy and is used to treat systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA). It exhibits immunomodulatory, antithrombotic, and antiplatelet properties. It inhibits the release endothelin-1, a potent vasoconstrictor, and restores impaired angiogenesis in TNF-α-treated endothelial cells in vitro. It also reduces the production of inflammatory cytokines such as TNF-α, IFN-γ, and IL-6 from peripheral blood mononuclear cells, upregulates IL-10 and decreases platelet aggregation.
Cancer Lett, 2024, 596:217009
Int J Mol Sci, 2022, 23(22)14149
S5973 Methylprednisolone Acetate Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
E4809New Piperaquine tetraphosphate tetrahydrate Piperaquine tetraphosphate tetrahydrate is an inhibitor of autophagy . It is a bisquinoline antimalarial agent effective against Plasmodium falciparum. Piperaquine tetraphosphate tetrahydrate is useful in antimalarial research.
S8744 PHY34 PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
S9424 Liensinine diperchlorate Liensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor.
E1232 Concanavalin A Concanavalin A is a potential anti-neoplastic agent targeting apoptosis, autophagy and anti-angiogenesis for cancer therapeutics.
S1078 MK-2206 2HCl MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.
Nat Cancer, 2024,
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
Nat Commun, 2024, 15(1):2132
S1039 Rapamycin Rapamycin is a specific mTOR inhibitor with IC50 of ~0.1 nM in HEK293 cells.Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator and an immunosuppressant.
Cancer Cell, 2024, S1535-6108(24)00350-7
Drug Resist Updat, 2024, 73:101063
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
S2673 Trametinib (GSK1120212) Trametinib (GSK1120212, JTP-74057) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib activates autophagy and induces apoptosis.
Nature, 2024, 629(8013):927-936
Cell, 2024, 187(3):712-732.e38
Cell, 2024, S0092-8674(24)00825-0
S1060 Olaparib (AZD2281) Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Cell, 2024, 187(4):945-961.e18
S1049 Y-27632 2HCl Y-27632 2HCl is a selective ROCK1 and ROCK2 inhibitor with a Ki of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Neural Regen Res, 2025, 20(1):242-252
Nature, 2024, 627(8004):594-603
Nature, 2024, 628(8009):818-825
S1263 Laduviglusib (CHIR-99021) Laduviglusib (CHIR-99021, CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.
Cell Stem Cell, 2024, S1934-5909(24)00256-X
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Protein Cell, 2024, pwae031
S1120 Everolimus Everolimus is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.
Cell, 2024, 187(3):712-732.e38
Cell, 2024, 187(3):712-732.e38
Kidney Int, 2024, S0085-2538(24)00627-6
S1025 Gefitinib Gefitinib is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Nature, 2024, 631(8020):424-431
Signal Transduct Target Ther, 2024, 9(1):65
Nat Genet, 2024, 10.1038/s41588-024-01948-8
S1166 Cisplatin Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
Int J Mol Med, 2025, 55(1)17
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
Nat Commun, 2024, 15(1):5775
S1267 Vemurafenib (PLX4032) Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.
Cell, 2024, 187(14):3652-3670.e40
Nat Commun, 2024, 15(1):4108
Nat Commun, 2024, 15(1):4108
S1378 Ruxolitinib Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Nat Commun, 2024, 15(1):2503
Nat Commun, 2024, 15(1):8663
Nat Commun, 2024, 15(1):2989
S1023 Erlotinib HCl Erlotinib HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Cell Discov, 2024, 10(1):39
J Extracell Vesicles, 2024, 13(7):e12494
Cell Mol Gastroenterol Hepatol, 2024, S2352-345X(24)00119-X
S7786 Erlotinib Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
Signal Transduct Target Ther, 2024, 9(1):65
Mol Cancer, 2024, 23(1):48
Nat Commun, 2024, 15(1):2742
S8048 Venetoclax (ABT-199) Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.
Nature, 2024,
Nat Immunol, 2024, 10.1038/s41590-024-01952-4
J Hematol Oncol, 2024, 17(1):85
S1047 Vorinostat (SAHA) Vorinostat (SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Cell Rep, 2024, 43(1):113575
NPJ Precis Oncol, 2024, 8(1):52
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
S1021 Dasatinib Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
Nature, 2024, 627(8003):407-415
Nature, 2024, 10.1038/s41586-024-07079-8
Mol Cancer, 2024, 23(1):240
S1250 Enzalutamide Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Acta Pharm Sin B, 2024, 14(6):2685-2697
Cell Rep Med, 2024, 5(2):101388
Cancer Lett, 2024, 597:217068
S7397 Sorafenib Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
J Hematol Oncol, 2024, 17(1):78
Cell Rep Med, 2024, S2666-3791(24)00201-5
J Exp Clin Cancer Res, 2024, 43(1):143
S7306 Dorsomorphin 2HCl Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.
Nat Commun, 2024, 15(1):4124
Nat Commun, 2024, 15(1):4124
Adv Sci (Weinh), 2024, 11(4):e2304987
S2111 Lapatinib Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
Drug Resist Updat, 2024, 73:101066
J Extracell Vesicles, 2024, 13(7):e12494
Cancer Lett, 2024, 593:216968
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
J Clin Invest, 2024, 134(18)e179860
Haematologica, 2024, 109(6):1713-1725
S1065 Pictilisib (GDC-0941) Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.
Nature, 2024, 10.1038/s41586-024-08031-6
Nat Genet, 2024, 10.1038/s41588-024-01948-8
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
S1068 Crizotinib Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Cancer Discov, 2024, OF1-OF20.
Nat Commun, 2024, 15(1):1009
Nat Commun, 2024, 15(1):51
S7840 Dorsomorphin Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For cell testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.
Nat Commun, 2024, 15(1):8547
J Clin Invest, 2024, 134(22)e181314
Nucleic Acids Res, 2024, gkae707
S1053 Entinostat (MS-275) Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Nat Commun, 2024, 15(1):4739
Nat Commun, 2024, 15(1):8044
J Clin Invest, 2024, 134(6)e171063
S1030 Panobinostat (LBH589) Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Nat Commun, 2024, 15(1):4450
Nat Commun, 2024, 15(1):5209
Emerg Microbes Infect, 2024, 13(1):2327371
S1011 Afatinib Afatinib inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
Cell, 2024, 187(3):712-732.e38
Cell, 2024, S0092-8674(24)00825-0
Signal Transduct Target Ther, 2024, 9(1):65
S7110 (+)-JQ1 (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Nat Immunol, 2024, 25(9):1580-1592
Gastroenterology, 2024, S0016-5085(24)00062-3
ACS Nano, 2024, 18(39):26614-26630
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Nat Commun, 2024, 15(1):1041
Cell Rep Med, 2024, 5(3):101471
Redox Biol, 2024, 72:103137
S1002 ABT-737 ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.
Gastroenterology, 2024, S0016-5085(24)00062-3
Nat Commun, 2024, 15(1):830
Nat Commun, 2024, 15(1):1041
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
Nat Cancer, 2024,
Nat Commun, 2024, 15(1):1300
Nat Commun, 2024, 15(1):7455
S1225 Etoposide Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis.
Nature, 2024, 635(8037):201-209
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
Nat Commun, 2024, 15(1):9181
S2475 Imatinib Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Nat Biomed Eng, 2024, 10.1038/s41551-024-01204-8
Cell Rep Med, 2024, S2666-3791(24)00201-5
Elife, 2024, 12RP92324
S2226 Idelalisib (CAL-101) Idelalisib (CAL-101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.
Cancer Immunol Res, 2024, 10.1158/2326-6066.CIR-23-1092
Transl Oncol, 2024, 43:101857
J Cell Commun Signal, 2024, 18(1):e12017
S1040 Sorafenib tosylate Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Nature, 2024, 629(8013):927-936
Cell Mol Life Sci, 2024, 81(1):238
J Transl Med, 2024, 22(1):593
S1555 AZD8055 AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.
Gastroenterology, 2024, S0016-5085(24)00062-3
Nat Commun, 2024, 15(1):2581
Nat Commun, 2024, 15(1):7675
S1714 Gemcitabine Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.
Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
Drug Resist Updat, 2024, 74:101079
Nat Commun, 2024, 15(1):1287
S1026 Imatinib Mesylate Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
Mol Cancer, 2024, 23(1):240
Cell Rep, 2024, 43(3):113811
JCI Insight, 2024, 9(10):e162449.
S1004 Veliparib (ABT-888) Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Cell Rep, 2024, 43(5):114205
S7781 Sunitinib Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Cell Rep Med, 2024, S2666-3791(24)00201-5
Pharmaceuticals (Basel), 2024, 17(1)77
Heliyon, 2024, 10(3):e24779
S2827 Torin 1 Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.
Mol Cell, 2024, S1097-2765(24)00832-3
Mol Cell, 2024, 84(8):1527-1540.e7
EMBO J, 2024,
S2853 Carfilzomib (PR-171) Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
Nature, 2024, 626(8000):874-880
J Hematol Oncol, 2024, 17(1):85
Nat Commun, 2024, 15(1):2207
S1224 Oxaliplatin Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
Mol Cancer, 2024, 23(1):186
Mol Cancer, 2024, 23(1):23
Gastroenterology, 2024, S0016-5085(24)00062-3
S1178 Regorafenib Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.
Nat Med, 2024, 10.1038/s41591-024-02824-y
Nature, 2024, 629(8011):450-457
Cell Rep Med, 2024, S2666-3791(24)00201-5
S1237 TMZ(Temozolomide) TMZ(Temozolomide) is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity.
Cell Discov, 2024, 10(1):39
Cell Death Dis, 2024, 15(3):205
NPJ Precis Oncol, 2024, 8(1):59
S5243 Ruxolitinib Phosphate Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Virol J, 2024, 21(1):23
Int J Mol Sci, 2023, 24(7)6228
Front Oncol, 2023, 13:1043694
S1130 Sepantronium Bromide (YM155) Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.
Cell Commun Signal, 2024, 22(1):440
Sci Rep, 2024, 14(1):7604
Adv Sci (Weinh), 2023, 10(25):e2301753
S1129 SRT1720 HCl SRT1720 HCl is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3. SRT1720 induces autophagy.
Int J Mol Sci, 2024, 25(17)9707
Int Immunopharmacol, 2024, 143(Pt 2):113521
Mol Pain, 2024, 20:17448069241232349
S1077 SB202190 SB202190 is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Nat Commun, 2024, 15(1):4124
Nat Commun, 2024, 15(1):5874
Nat Commun, 2024, 15(1):4124
S1149 Gemcitabine HCl Gemcitabine HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.
Int J Biol Sci, 2024, 20(4):1389-1409
Phytomedicine, 2024, 155377
NPJ Precis Oncol, 2024, 8(1):246
S7810 Afatinib Dimaleate Afatinib Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.
Cell, 2024, 187(3):712-732.e38
Signal Transduct Target Ther, 2024, 9(1):153
J Invest Dermatol, 2024, S0022-202X(23)03210-4
S1582 H 89 2HCl H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy.
Nat Commun, 2024, 15(1):8887
J Extracell Vesicles, 2024, 13(4):e12426
J Extracell Vesicles, 2024, 13(4):e12426
S1191 Fulvestrant Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.
Cancer Lett, 2024, 593:216968
Cell Death Dis, 2024, 15(8):590
Cell Death Dis, 2024, 15(7):480
S2449 Forskolin (Colforsin) Forskolin (Colforsin) is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types, commonly used to raise levels of cAMP in the study and research of cell physiology. Forskolin also activates PXR and FXR activity. Forskolin stimulates autophagy.
Circulation, 2024, 149(18):1435-1456
Cell Stem Cell, 2024, S1934-5909(24)00048-1
Sci Bull (Beijing), 2024, S2095-9273(24)00799-0
S1033 Nilotinib Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Nat Commun, 2024, 15(1):651
Nat Commun, 2024, 15(1):2089
Elife, 2024, 12RP92324
S2248 Silmitasertib (CX-4945) Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.
Diabetologia, 2024, 10.1007/s00125-024-06128-1
Biomed Pharmacother, 2024, 180:117499
Front Immunol, 2024, 15:1393485
S1141 Tanespimycin (17-AAG) Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
Cell, 2024, S0092-8674(24)00583-X
Cell, 2024, S0092-8674(24)00583-X
Theranostics, 2024, 14(6):2442-2463
S1014 Bosutinib Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
Elife, 2024, 12RP92324
Front Immunol, 2024, 15:1425670
PLoS Pathog, 2024, 20(7):e1012170
S1048 Tozasertib (VX-680) Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.
Cell Death Dis, 2024, 15(1):56
Cell Rep, 2024, 43(9):114739
Elife, 2024, 12RP92324
S1230 Flavopiridol (Alvocidib) Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.
Nat Commun, 2024, 15(1):5151
Nat Commun, 2024, 15(1):8539
Nat Commun, 2024, 15(1):35
S2929 Pifithrin-α (PFTα) HBr Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).
Cell Death Differ, 2024, 31(8):999-1012
Int J Biol Sci, 2024, 20(6):2008-2026
Cell Mol Life Sci, 2024, 81(1):101
S1057 Obatoclax Mesylate (GX15-070) Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Emerg Microbes Infect, 2022, 1-29
Cancers (Basel), 2022, 14(22)5602
S1046 Vandetanib Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
Front Pharmacol, 2024, 15:1345070
Front Pharmacol, 2024, 15:1345070
S1122 Mocetinostat (MGCD0103) Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.
Dev Cell, 2024, S1534-5807(24)00326-5
J Invest Dermatol, 2024, S0022-202X(23)03210-4
Clin Epigenetics, 2024, 16(1):13
S1069 Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Cell Commun Signal, 2024, 22(1):397
Sci Adv, 2024, 10(8):eadk3663
bioRxiv, 2024, 10.1101/2024.01.16.575190
S1782 Azacitidine (5-Azacytidine) Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.
J Hematol Oncol, 2024, 17(1):85
Nat Commun, 2024, 15(1):7360
Nat Commun, 2024, 15(1):4739
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Cancers (Basel), 2024, 16(13)2447
bioRxiv, 2024, 2024.02.19.581073
J Transl Med, 2023, 21(1):89
S1044 Temsirolimus Temsirolimus is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
ACS Nano, 2024, 18(45):31451-31465
Cell Commun Signal, 2024, 22(1):428
iScience, 2024, 27(6):109817
S1085 Belinostat Belinostat is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.
Nat Commun, 2024, 15(1):4739
J Immunother Cancer, 2024, 12(10)e009590
Cell Rep, 2024, 43(1):113575
S2218 Torkinib (PP242) Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and apoptosis.
Mol Cell, 2024, S1097-2765(24)00832-3
Cell Death Dis, 2024, 15(1):48
Mol Oncol, 2024, 10.1002/1878-0261.13716
S7152 C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.
Nat Commun, 2024, 15(1):5209
Cell Commun Signal, 2024, 22(1):117
Antioxidants (Basel), 2024, 13(4)424
S1322 Dexamethasone Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.
Cell Host Microbe, 2024, S1931-3128(24)00005-2
Nat Commun, 2024, 15(1):7991
Nat Commun, 2024, 15(1):1176
S8075 GANT61 GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.
EBioMedicine, 2024, 101:105026
Cell Death Dis, 2024, 15(10):739
Acta Pharm Sin B, 2023, 13(6):2601-2612
S1075 SB216763 SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB216763 activates autophagy.
Sci Rep, 2024, 14(1):11174
SLAS Discov, 2024, 29(8):100191
Leukemia, 2023, 37(8):1611-1625
S8049 Tubastatin A Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
Theranostics, 2024, 14(6):2345-2366
Biomedicines, 2024, 12(6)1203
Life Sci Alliance, 2024, 7(7)e202302384
S5003 Tacrolimus (FK506) Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
Nat Immunol, 2024, 25(5):860-872
Int J Antimicrob Agents, 2024, 63(5):107116
Cell Commun Signal, 2024, 22(1):428
S1950 Metformin HCl Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Nat Commun, 2024, 15(1):1785
J Clin Invest, 2024, e175023
EBioMedicine, 2024, 102:105090
S7007 Binimetinib (MEK162) Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.
Nature, 2024, 629(8013):927-936
Signal Transduct Target Ther, 2024, 9(1):293
Gastroenterology, 2024, S0016-5085(24)00062-3
S2783 Vistusertib (AZD2014) Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
Cell Rep Med, 2023, 4(4):101007
Front Pharmacol, 2023, 14:1158775
Cancers (Basel), 2023, 15(13)3451
S7655 Telaglenastat (CB-839) Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1.
Nat Commun, 2024, 15(1):9820
Nat Commun, 2024, 15(1):5620
EBioMedicine, 2024, 102:105090
S2626 Rabusertib (LY2603618) Rabusertib (LY2603618, IC-83) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
Cell, 2024, 187(14):3652-3670.e40
Mol Cell, 2024, S1097-2765(24)00285-5
Neoplasia, 2024, 57:101038
S1648 Cytarabine Cytarabine is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.
Nat Commun, 2024, 15(1):4739
Nat Commun, 2024, 15(1):9820
Blood Adv, 2024, 8(20):5315-5329
S1233 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines.
Theranostics, 2024, 14(13):5123-5140
Int J Biol Sci, 2024, 20(6):2323-2338
J Transl Med, 2024, 22(1):649
S8059 Nutlin-3a Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.
EMBO J, 2024, 10.1038/s44318-024-00240-z
J Neuroinflammation, 2024, 21(1):57
Front Immunol, 2024, 15:1374943
S1573 Fasudil HCl Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
J Immunother Cancer, 2024, 12(11)e009805
Sci China Life Sci, 2024, 67(8):1549-1562
CNS Neurosci Ther, 2024, 30(11):e70098
S3012 Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
Cell Rep Med, 2024, S2666-3791(24)00201-5
Biomed Pharmacother, 2024, 180:117468
Transl Psychiatry, 2024, 14(1):166
S5742 Deferoxamine mesylate Deferoxamine mesylate is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy.Please do not prepare stock solutions with normal saline or PBS, as precipitation may occur.
Mol Cancer, 2024, 23(1):240
Cancer Commun (Lond), 2024, 10.1002/cac2.12608
Adv Sci (Weinh), 2024, 11(40):e2402671
S1017 Cediranib (AZD2171) Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.
Front Oncol, 2024, 14:1302850
Cell Oncol (Dordr), 2023, 46(2):391-407
Cell Oncol (Dordr), 2023, 46(2):391-407
S2180 Ixazomib (MLN2238) Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Ixazomib (MLN2238) induces autophagy. Phase 3.
Sci Rep, 2024, 14(1):18772
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
iScience, 2023, 26(8):107302
S4908 SN-38 SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.
Cell, 2024, 187(20):5698-5718.e26
Nat Commun, 2024, 15(1):2503
Cell Rep Med, 2024, 5(7):101627
S7409 Anisomycin Anisomycin (Flagecidin, Wuningmeisu C) is a bacterial antibiotic isolated from Streptomyces griseolus, which inhibits protein synthesis, and also act as a JNK activator. Anisomycin upregulates autophagy and increases apoptosis.
Theranostics, 2024, 14(4):1561-1582
Research (Wash D C), 2024, 7:0331
Acta Biomater, 2024, S1742-7061(24)00036-9
S1396 Resveratrol Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
Biochem Biophys Res Commun, 2024, 723:150186
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
S2285 Cryptotanshinone (Tanshinone C) Cryptotanshinone (Tanshinone C) is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
Bone Joint Res, 2024, 13(4):137-148
J Med Virol, 2023, 95(11):e29230
Microbiol Spectr, 2023, e0493222.
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Nat Commun, 2024, 15(1):7675
Microorganisms, 2024, 12(2)296
Autophagy, 2023, 19(11):2912-2933
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Cancer Discov, 2023, 13(3):598-615
Nat Commun, 2023, 14(1):2829
Cancer Res Commun, 2023, 3(4):659-671
S1792 Simvastatin Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.
J Immunother Cancer, 2024, 12(11)e009805
Cancer Med, 2024, 13(12):e7393
Neuron, 2023, S0896-6273(23)00513-5
S2556 Rosiglitazone Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Nat Commun, 2024, 15(1):1429
Nat Commun, 2024, 15(1):7991
Research (Wash D C), 2024, 7:0400
S1080 SU11274 SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.
Cancer Cell Int, 2024, 24(1):43
J Transl Med, 2023, 21(1):530
J Transl Med, 2023, 21(1):530
S2799 Daporinad (FK866) Daporinad (FK866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.
Cell Discov, 2024, 10(1):39
Theranostics, 2024, 14(7):2794-2815
Theranostics, 2024, 14(15):5999-6015
S1035 Pazopanib HCl Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.
iScience, 2023, 26(7):107116
NPJ Breast Cancer, 2022, 8(1):44
J Pers Med, 2022, 12(2)258
S2679 Flavopiridol (Alvocidib) HCl Flavopiridol (Alvocidib) HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.
Elife, 2024, 13e80684
Int J Biol Macromol, 2023, 258(Pt 1):128776
Mol Cell Biol, 2023, 43(1):1-21
S2658 Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1.
Mol Cancer, 2024, 23(1):78
Mol Cancer, 2024, 23(1):78
JCI Insight, 2024, 9(10)e164191
S1238 Tamoxifen Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
Nat Commun, 2024, 15(1):2377
Breast Cancer Res, 2024, 26(1):33
Toxics, 2024, 12(4)247
S1314 Zoledronic acid (Zoledronate) Zoledronic acid (Zoledronate), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
Cells, 2024, 13(10)862
Cells, 2024, 13(10)862
Cancer Immunol Immunother, 2024, 73(4):62
S2843 BI-D1870 BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.
Cells, 2024, 13(18)1546
Sci Rep, 2024, 14(1):9440
BMC Cancer, 2024, 24(1):233
S2163 PF-4708671 PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. PF-4708671 induces autophagy. First S6K1-specific inhibitor to be reported.
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
Int J Mol Sci, 2024, 25(7)3944
Am J Cancer Res, 2024, 14(3):1087-1100
S7164 GSK343 GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy.
Cancers (Basel), 2024, 16(9)1639
Sci Adv, 2024, 10(13):eadk4423
J Immunother Cancer, 2023, 11(11)e007736
S7130 PR-619 PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM in a cell-free assay. PR-619 activates autophagy.
Nat Commun, 2024, 15(1):1642
Mol Cell, 2024, 84(16):3115-3127.e11
BMC Biol, 2024, 22(1):71
S8047 Dynasore Dynasore is a cell-permeable, reversible non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2, with IC50 of 15 μM in a cell-free assay, also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase. Dynasore suppresses mTORC1 activity and induces autophagy. Dynasore inhibits the entry of several viruses, including herpes simplex virus (HSV).
Immunity, 2024, 57(2):287-302.e12
Nat Commun, 2024, 15(1):1669
Redox Biol, 2024, 76:103335
S7842 LY3009120 LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.
Drug Resist Updat, 2023, 71:100993
Exp Cell Res, 2023, 430(1):113722
Curr Issues Mol Biol, 2023, 45(7):5865-5878
S1190 Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
iScience, 2024, 27(3):109246
Cancers (Basel), 2024, 16(7)1303
Cancers (Basel), 2024, 16(2)296
S2061 Lovastatin Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM in a cell-free assay, used for lowering cholesterol (hypolipidemic agent). Lovastatin triggers autophagy.
Cell Discov, 2024, 10(1):39
Nat Commun, 2024, 15(1):6740
Int J Biol Sci, 2024, 20(6):2130-2148
S1590 TWS119 TWS119 is a GSK-3β inhibitor with IC50 of 30 nM in a cell-free assay; capable of inducing neuronal differentiation and may be useful to stem cell biology. GSK-3β inhibition triggers autophagy.
Nat Commun, 2024, 15(1):2089
Sci Rep, 2024, 14(1):5038
SLAS Discov, 2024, 29(8):100191
S1228 Idarubicin HCl Idarubicin HCl (4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy.
Cell Rep, 2024, 43(7):114388
BMC Pharmacol Toxicol, 2024, 25(1):25
Mol Cell, 2023, 83(13):2206-2221.e11
S1231 Topotecan HCl Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.
Mol Cell, 2024, 84(14):2618-2633.e10
Cancer Cell Int, 2024, 24(1):285
iScience, 2024, 27(1):108667
S2219 Momelotinib (CYT387) Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
Cell Rep, 2023, 42(9):113067
Breast Cancer Res, 2023, 25(1):51
S7998 Entrectinib Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
Signal Transduct Target Ther, 2024, 9(1):153
Biomed Pharmacother, 2024, 176:116766
J Pathol, 2024, 263(2):257-269
S3030 Niclosamide Niclosamide can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5).
PLoS Pathog, 2024, 20(7):e1012352
Int J Nanomedicine, 2023, 18:7505-7521
Front Cell Dev Biol, 2023, 11:1062229
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Elife, 2024, 12RP92324
Sci Rep, 2024, 14(1):4303
Environ Mol Mutagen, 2024, 10.1002/em.22604
S2198 SGI-1776 free base SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. SGI-1776 induces apoptosis and autophagy.
Cell Death Dis, 2024, 15(9):644
Mar Drugs, 2024, 22(10)444
Mol Cancer, 2023, 22(1):64
S8006 BIX 01294 BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.
Acta Pharm Sin B, 2024, 14(3):1187-1203
Cell Commun Signal, 2024, 22(1):402
Dev Cell, 2023, 58(6):506-521.e5
S1135 Pemetrexed disodium Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
Cell Death Dis, 2024, 15(8):555
Cell Commun Signal, 2024, 22(1):375
Cancer Cell, 2022, 40(10):1128-1144.e8
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Cancer Cell Int, 2024, 24(1):303
Front Pharmacol, 2024, 15:1418902
PLoS Negl Trop Dis, 2024, 18(8):e0012428
S7483 DMOG DMOG (Dimethyloxalylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy.Solutions are unstable and should be fresh-prepared.
Life Sci Alliance, 2025, 8(1)e202403053
Nat Cell Biol, 2024, 10.1038/s41556-024-01475-y
Immunology, 2024, 10.1111/imm.13797
S1896 Hydroxyurea Hydroxyurea is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.
Nature, 2024, 635(8037):201-209
Nat Commun, 2024, 15(1):7360
iScience, 2024, 27(4):109580
S2624 OSI-027 OSI-027 (ASP4786, CERC 006, AEVI-006) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. OSI-027 induces autophagy in cancer cells.
J Cell Commun Signal, 2023, 17(3):975-989
Emerg Microbes Infect, 2022, 11(1):519-531
Mol Carcinog, 2022, 10.1002/mc.23414
S2476 Itraconazole Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Cell Infect Microbiol, 2023, 13:1131641
Front Cell Infect Microbiol, 2022, 12:864912
S2391 Quercetin Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
Cell Metab, 2024, S1550-4131(24)00371-1
Nucleic Acids Res, 2024, gkae322
Clin Transl Med, 2024, 14(5):e1660
S4505 Vinblastine sulfate Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.
Int J Mol Sci, 2024, 25(21)11346
PLoS One, 2024, 19(11):e0307153
Nat Commun, 2023, 14(1):7576
S4269 Vinorelbine ditartrate Vinorelbine ditartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin. Vinorelbine Tartrate exhibits anti-tumor activities via inducing the mitotic apoptosis, autophagy and inflammation.
Cell Death Dis, 2024, 15(8):603
BMC Pharmacol Toxicol, 2024, 25(1):25
BMC Pharmacol Toxicol, 2024, 25(1):25
S1235 Letrozole Letrozole is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM in cell-free assays.It has no effect on the plasma levels of 17α-OH progesterone, thyroid-stimulating hormone (TSH), luteinizing hormone (LH), follicle-stimulating hormone (FSH), or androstenedione and does not affect normal urine electrolyte excretion or thyroid function in clinical studies. Letrozole induces autophagy.
eNeuro, 2024, 11(8)ENEURO.0332-24.2024
J Chromatogr B Analyt Technol Biomed Life Sci, 2024, 1238:124106
Mol Oncol, 2023, 10.1002/1878-0261.13541
S2770 MK-5108 MK-5108 is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. MK-5108 (VX-689) induces autophagy. Phase 1.
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
Sci Rep, 2024, 14(1):4303
Biosensors (Basel), 2022, 12(4)196
S7104 AZD1208 AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.
Angiogenesis, 2024, 10.1007/s10456-024-09906-y
Cell Death Dis, 2024, 15(4):274
Inflamm Res, 2024, 10.1007/s00011-024-01924-2
S7785 Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. Pemetrexed Disodium Hydrate stimulates autophagy and apoptosis.
Cell Rep, 2022, 38(9):110448
Front Pharmacol, 2022, 13:1032975
J Pers Med, 2022, 12(2)258
S2713 Geldanamycin Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.
Nat Commun, 2024, 15(1):9448
Cell Rep, 2024, 43(10):114827
Int J Mol Sci, 2023, 24(18)13830
S1003 Linifanib (ABT-869) Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.
Cell Death Discov, 2023, 9(1):57
Cell Death Discov, 2023, 9(1):57
Cancer Cell, 2022, S1535-6108(22)00312-9
S1168 Valproic Acid sodium Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
J Exp Clin Cancer Res, 2024, 43(1):152
J Immunother Cancer, 2024, 12(11)e009805
Sci Total Environ, 2022, 838(Pt 2):155825
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
Mol Oncol, 2024, 10.1002/1878-0261.13577
Cell Metab, 2022, S1550-4131-2200411-9
S2635 CCT128930 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of CCT128930 triggers cell apoptosis in HepG2 cells.
Nat Commun, 2024, 15(1):6150
Cell Rep, 2024, 43(4):114108
Nat Commun, 2023, 14(1):886
S3944 VPA (Valproic acid) VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.
Sci Bull (Beijing), 2024, S2095-9273(24)00799-0
Nat Commun, 2024, 15(1):668
Dev Cell, 2024, S1534-5807(24)00326-5
S2310 Honokiol Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Honokiol causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. Honokiol inhibits hepatitis C virus (HCV) infection. Phase 3.
Int J Nanomedicine, 2023, 18:4313-4327
Exp Gerontol, 2023, 173:112091
Cell Death Differ, 2022, 10.1038/s41418-022-01053-5
S4028 Dexamethasone Sodium Phosphate Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
Cancer Cell, 2024, 42(9):1507-1527.e11
Pharmaceutics, 2022, 14(2)400
Front Oncol, 2022, 12:888695
S8078 Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
Nat Commun, 2024, 15(1):7249
Sci Rep, 2024, 14(1):22572
Nat Commun, 2023, 14(1):3648
S2782 GW4064 GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.
Gut Microbes, 2024, 16(1):2379566
Mol Metab, 2024, 79:101841
Chin Med, 2024, 19(1):16
S2505 Rosiglitazone maleate Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
S1999 Sodium butyrate Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). Sodium butyrate (NaB) inhibits cell cycle progression, promotes differentiation, and induces apoptosis and autophagy in several types of cancer cells.
Nat Commun, 2024, 15(1):4764
Nat Commun, 2024, 15(1):5209
Cell Rep, 2024, 43(2):113778
S7165 UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. UNC1999 is a potent autophagy inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis.
Nat Commun, 2024, 15(1):7366
Acta Pharm Sin B, 2023, 13(6):2601-2612
Acta Pharm Sin B, 2023, 13(6):2601-2612
S7177 PF-543 hydrochloride PF-543 hydrochloride, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
J Transl Med, 2024, 22(1):43
Int J Mol Sci, 2023, 24(9)8303
Cell Res, 2022, 10.1038/s41422-022-00614-0
S2290 DHA (Dihydroartemisinin) DHA (Dihydroartemisinin) is a semi-synthetic derivative of artemisinin and isolated from the traditional Chinese herb Artemisia annua. Dihydroartemisinin induces autophagy and apoptosis by suppressing NF-κB activation.
Int Immunopharmacol, 2024, 139:112637
Front Pharmacol, 2024, 15:1418902
ACS Infect Dis, 2024, 10.1021/acsinfecdis.3c00588
S7680 SP2509 SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.
Nat Commun, 2024, 15(1):5631
bioRxiv, 2024, 2024.05.19.594897
MedComm (2020), 2023, 4(3):e269
S3022 Cabazitaxel Cabazitaxel is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.
J Photochem Photobiol B, 2024, 253:112877
Cancer Biol Ther, 2024, 25(1):2329368
Sci Adv, 2024, 10(5):eadg7887
S2606 Mifepristone Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Neuron, 2024, S0896-6273(24)00089-8
Cell Death Dis, 2024, 15(1):70
Cell Death Dis, 2024, 15(1):73
S3017 Aspirin Aspirin is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin induces autophagy and stimulates mitophagy.
Cell Death Discov, 2023, 10.1038/s41420-023-01664-y
iScience, 2023, 26(7):107105
Comput Struct Biotechnol J, 2022, 20:5750-5760
S5971 Pemetrexed Pemetrexed (LY231514) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
Cell Rep Med, 2024, 5(7):101615
Mol Cancer Res, 2024, 22(1):82-93
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Cancer Cell, 2024, 42(4):535-551.e8
Sci Rep, 2024, 14(1):25682
Sci Rep, 2024, 14(1):879
S7215 Losmapimod Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.
Nat Commun, 2024, 15(1):987
Int J Mol Sci, 2024, 25(13)7302
J Radiat Res, 2024, rrae021
S1290 Celastrol Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.
Int J Biol Sci, 2024, 20(14):5731-5746
Int J Mol Sci, 2024, 25(10)5237
Fundam Res, 2024, 4(2):394-400
S5715 Atorvastatin Atorvastatin is a lipid lowering agent. It is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway. Atorvastatin activates autophagy.
MedComm (2020), 2024, 5(5):e525
Oncogene, 2024, 43(4):281-293
Mol Cancer, 2023, 22(1):147
S1759 Pitavastatin calcium Pitavastatin calcium, a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
Nat Commun, 2024, 15(1):4099
J Immunother Cancer, 2024, 12(11)e009805
Cell Rep, 2024, 43(6):114286
S1218 Clofarabine Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.
Front Oncol, 2023, 13:1287444
Cancer Res, 2022, 82(4):721-733
Clin Transl Med, 2022, 12(2):e747
S7134 IU1 IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μ M, 25-fold selective to IsoT. IU1 induces autophagy.
Redox Biol, 2024, 76:103318
Antioxidants (Basel), 2024, 13(1)114
Nat Commun, 2022, 13-1:5644
S1972 Tamoxifen Citrate Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.
bioRxiv, 2024, 2023.05.10.540211
RNA, 2023, 29(9):1325-1338.
RNA, 2023, rna.079509.122
S1312 STZ (Streptozotocin) STZ (Streptozotocin) is a glucosamine-nitrosourea compound derived from Streptomyces achromogenes, which is a DNA-methylating, carcinogenic, antibiotic and diabetes inducing agent. Streptozotocin induces autophagy and apoptosis. Streptozotocin (STZ) can be used to induce animal models of diabetes. Solutions are unstable and should be fresh-prepared.
Cell Commun Signal, 2024, 22(1):368
Fluids Barriers CNS, 2024, 21(1):26
CNS Neurosci Ther, 2024, 30(8):e14913
S7724 Eprenetapopt (APR-246) Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.
Oncotarget, 2024, 15:614-633
J Cell Mol Med, 2024, 28(9):e18374
Cell Death Dis, 2023, 14(11):783
S2812 (R)-(-)-Gossypol (AT-101) acetic acid (R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.
Protein Cell, 2024, pwad065
Int J Mol Sci, 2023, 24(7)6662
Cancer Cell, 2022, S1535-6108(22)00312-9
S3031 Linagliptin (GSK2118436) Linagliptin (GSK2118436) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells.
Pharmacol Res, 2024, 207:107298
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
J Pers Med, 2022, 12(2)258
S1576 Sulfasalazine Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Med Oncol, 2024, 41(8):188
Adv Sci (Weinh), 2023, 10(20):e2300517
Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
S7793 Purvalanol A Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy.
Biomacromolecules, 2024, 10.1021/acs.biomac.4c00672
Cancers (Basel), 2023, 10.3390/cancers15225424
Cancer Res, 2022, canres.1707.2021
S2751 Milciclib Milciclib is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7, it's also an inhibitor of TRKA with IC50 of 53nM. Milciclib (PHA-848125) induces cell death through autophagy. Phase 2.
medRxiv, 2023, 2023.11.13.23298409
Nat Commun, 2022, 13(1):2725
ProQuest, 2022, 29166130
S1219 YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy.
Mol Biol Cell, 2024, 35(5):ar70
Nat Commun, 2022, 13(1):2136
Blood Cancer J, 2022, 12(3):39
S1351 Ivermectin Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
J Clin Invest, 2024, 134(22)e181314
Viruses, 2024, 16(4)640
Life Sci Alliance, 2023, 6(8)e202302133
S7067 Tepotinib Tepotinib is a potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib (EMD 1214063) induces autophagy. Phase 1.
Oncogene, 2024, 10.1038/s41388-024-02987-5
Int J Mol Sci, 2024, 25(3)1769
Int J Mol Sci, 2024, 25(3)1769
S1847 Clemastine fumarate Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Glia, 2024, 72(9):1555-1571
Neurobiol Dis, 2024, 190:106375
J Clin Invest, 2022, e152187
S1794 Fenofibrate Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.
J Immunother Cancer, 2024, 12(11)e009805
Heliyon, 2024, 10(11):e31861
Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
S7343 URMC-099 URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
Cell Commun Signal, 2023, 21(1):82
Oncogene, 2023, 42(14):1132-1143.
Oncogenesis, 2023, 12(1):35
S1403 Tigecycline Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline induces autophagy by downregulating the PI3K-AKT-mTOR pathway.
Int J Mol Sci, 2024, 25(9)4887
Int J Mol Sci, 2024, 25(9)4887
Antimicrob Agents Chemother, 2024, 68(3):e0112023
S1979 Amiodarone HCl Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.
J Immunother Cancer, 2024, 12(11)e009805
Cell Rep Methods, 2023, 3(4):100440
Cell Rep Methods, 2023, 3(4):100440
S4895 Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Nat Commun, 2024, 15(1):2089
J Pharm Sci, 2022, 111(8):2180-2190
EMBO Mol Med, 2021, e11814
S2077 Atorvastatin Calcium Atorvastatin Calcium is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol. Atorvastatin Calcium induces apoptosis and autophagy.
J Immunother Cancer, 2024, 12(11)e009805
Cancers (Basel), 2022, 14(9)2327
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
S7684 Salirasib Salirasib (Farnesylthiosalicylic acid, FTS) is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Phase 2.
J Biol Chem, 2023, 299(4):103017
Microbiol Spectr, 2023, 11(4):e0055223
Nat Commun, 2022, 13(1):7113
S4211 Montelukast Sodium Montelukast Sodium selectively antagonizes leukotriene D4 (LTD4) by binding to it so that block the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1. Montelukast improves macroautophagy but not the chaperone-mediated autophagy pathway. Solutions are unstable and should be fresh-prepared.
Biochem Biophys Res Commun, 2022, 594:31-37
Cancer Immunol Immunother, 2021, 70(1):203-213
Aging (Albany NY), 2021, 13(24):25670-25693
S2480 Loperamide HCl Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease.
Front Neurosci, 2024, 18:1424936
Front Cell Infect Microbiol, 2023, 13:1139152
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
S1389 Omeprazole Omeprazole is a proton pump inhibitor that blocks H(+)-K(+)-ATPase, used to treat dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome.
J Extracell Vesicles, 2024, 13(4):e12426
J Extracell Vesicles, 2024, 13(4):e12426
J Transl Med, 2024, 22(1):676
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy.
Sci Rep, 2024, 14(1):8200
bioRxiv, 2023, 10.1101/2023.12.19.572304
Burns Trauma, 2020, 8:tkaa025
S4484 Trametinib DMSO solvate Trametinib DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis.
JID Innov, 2024, 4(2):100248
Cell Rep, 2022, 38(7):110374
Mol Cell Proteomics, 2022, 21(6):100240
S2181 Ixazomib Citrate (MLN9708) Analogue Ixazomib Citrate (MLN9708) Analogue is the analogue of Ixazomib Citrate (MLN9708) from WO2016165677A1. Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Ixazomib (MLN2238) induces autophagy. Phase 3.
EMBO J, 2023, 42(17):e111719
iScience, 2023, 26(6):106997
J Dermatol Sci, 2022, S0923-1811(22)00125-6
S1693 Carbamazepine Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
J Immunother Cancer, 2024, 12(11)e009805
mBio, 2022, e0217721
Front Pharmacol, 2021, 12:749930
S7648 OTS964 OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts.
Nucleic Acids Res, 2023, gkad001
Cancer Lett, 2022, 544:215812
Cell Death Dis, 2022, 13(5):450
S8240 SMER28 SMER28 is a small-molecule enhancer (SMER) of autophagy, inducing autophagy independently of rapamycin in mammalian cells.
Nat Chem Biol, 2020, 6
Cell Rep, 2020, 31(12):107800
Cell Rep, 2019, 27(12):3413-3421
S1747 Nimodipine Nimodipine (BAY E 9736) is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.
J Immunother Cancer, 2024, 12(11)e009805
Eye Vis (Lond), 2024, 11(1):37
Cell Discov, 2020, 6(1):96
S3653 Spermidine trihydrochloride Spermidine (4-Azaoctamethylenediamine), a natural polyamine produced from putrescine and decarboxylated S-adenosylmethionine (dcSAM) by spermidine synthase, is a novel autophagy inducer and negatively modulates N-methyl-d-aspartate (NMDA).
Cell Metab, 2023, S1550-4131(23)00341-8
Int J Mol Sci, 2021, 22(19)10255
Int J Mol Sci, 2021, 22(19), 10255
S8432 Troglitazone Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
CNS Neurosci Ther, 2024, 30(8):e14911
Int J Mol Med, 2024, 53(4)37
Free Radic Biol Med, 2021, 163:234-242
S1837 Flubendazole Flubendazole (Flumoxanal, NSC 313680) is an autophagy inducer by targeting Atg4B, used to treat internal parasite and worm infection.
Nat Commun, 2024, 15(1):4513
Sci Rep, 2020, 10(1):13124
RSC Advances, 2018, 10.1039/C7RA12259D
S0709 Tubastatin A TFA Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
Cell Mol Life Sci, 2023, 80(11):333
Cell Mol Life Sci, 2023, 80(11):333
Drug Dev Res, 2022, 10.1002/ddr.21927
S6650 EN6 EN6 is a novel covalent autophagy activator and targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase with an IC50 of 1.7 μM for recombinant human ATP6V1A protein.
Cell Death Dis, 2021, 12(1):119
Life (Basel), 2021, 11(9)948
Brain Res, 2021, 1778:147768
S6847 ML-9 HCl ML-9 HCl (ML-9 hydrochloride) is a selective and potent inhibitor of Akt kinase, myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). ML-9 HCl is also a potent inhibitor of Ca2+-permeable channels. ML-9 HCl is a lysosomotropic agent targeting autophagy and cell death.
PLoS Pathog, 2023, 19(3):e1011295
J Mol Endocrinol, 2019, 63(3):199-213
S6301 MPP+ iodide MPP+ iodide (N-Methyl-4-Phenylpyridinium Iodide), the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces autophagic cell death in SH-SY5Y cells. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA) neurons, but internalization of serotonin transporter (SERT) in serotonergic (5-HT) neurons.
Front Immunol, 2023, 14:1193081
Front Immunol, 2023, 14:1193081
S2458 Clonidine HCl Clonidine HCl(Kapvay) is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg.
J Immunother Cancer, 2024, 12(11)e009805
Mol Pain, 2022, 18:17448069221107810
S8943 VLX600 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity.
Cancers (Basel), 2022, 14(13)3225
S6797 QX77 QX77 is a novel activator of chaperone-mediated autophagy (CMA). QX77 induces the up-regulation of Rab11 expression and up-regulates LAMP2A expression.
Autophagy, 2024, 10.1080/15548627.2024.2395797
Front Pharmacol, 2021, 12:707259
S6919 Brevilin A Brevilin A (6-O-Angeloylplenolina), a sesquiterpene lactone isolated from Centipeda minima, is a selective inhibitor of STAT3 and attenuates the JAKs activity by blocking the JAKs tyrosine kinase domain JH1. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.
Front Pharmacol, 2022, 13:795613
S4081 Sulfacetamide Sodium Sulfacetamide Sodium is an anti-biotic.
G3 (Bethesda), 2020, 4;10(5):1585-1597
S6078 ICCB-19 hydrochloride ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy.
Cell Death Discov, 2023, 9(1):109
S6395 CA77.1 CA77.1 (CA) is a potent, brain-penetrant and orally active activator of chaperone-mediated autophagy (CMA) for the treament of Alzheimer's disease (AD).
Sci Adv, 2023, 9(40):eadi8343
S2491 Nitrendipine Nitrendipine (Bayotensin) is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.
Nat Commun, 2024, 15(1):8708
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis.
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S1027 FL-411 FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction.
S8964 Actinomycin D (Dactinomycin) Actinomycin D (Dactinomycin, Act D, RASP-101) is a significant polypeptide antibiotic isolated from soil bacteria of the genus Streptomyces. Actinomycin D (Dactinomycin) inhibits DNA repair and rests the cell cycle at G1 phase with IC50 of 0.42 μM and 0.4 nM, respectively. Actinomycin D is an autophagy activator, induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
Mol Cancer, 2024, 23(1):186
Nat Commun, 2024, 15(1):5209
Exp Mol Med, 2024, 10.1038/s12276-024-01315-x
S6957 β-Elemene

β-Elemene ((-)-β-Elemene, Levo-β-elemene) is a sesquiterpene compound extracted from the herb Curcuma Rhizoma with antitumor activities. β-elemene can inhibit cell proliferation, arrest the cell cycle, and induce cell apoptosis or autophagy.

S9027 Corynoxine Corynoxine, a natural oxindole alkaloid, is a new autophagy enhancer.
S9860 BC1618 BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.
S9611 ABTL-0812 ABTL0812 (α-Hydroxylinoleic acid, LP-10218, SCLN-0812) inhibits Akt/mTOR axis by inducing the overexpression of TRIB3 and activating autophagy in lung squamous carcinoma cell lines. ABTL0812 also induces AMPK activation and ROS accumulation.
S4476 PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells.
S6851 RA-190 RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.
S3569 Spermidine Spermidine is a natural polyamine that stimulates cytoprotective macroautophagy/autophagy.
Cell Metab, 2023, S1550-4131(23)00341-8
Oxid Med Cell Longev, 2022, 2022:8033353
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
S4546 Xylitol Xylitol (Adonitol, Ribitol, Xylite, D-Xylitol, Adonite) is a sugar alcohol derived from XYLOSE by reduction of the carbonyl group. It is as sweet as sucrose and used as a noncariogenic sweetener.
S0012 E260 E260 (Fer and FerT inhibitor E260) is a Fer kinase and FerT inhibitor that selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level.
S9310 Isorhychophylline Isorhynchophylline (IsoRhy, 7-Isorhyncophylline) is a major tetracyclic oxindole alkaloid isolated from the Chinese herbal medicine Uncaria rhynchophylla (Miq.)Jacks (Gouteng in Chinese). It acts as a neuronal autophagy inducer with therapeutic potential for cardiovascular and central nervous system diseases.
S7307 GSK2606414 GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. GSK2606414 impairs GANT-61 induced autophagy in NB cells with MYCN amplification. GSK2606414 exacerbates ER stress-induced apoptosis in HCT116 cells while reduces the apoptosis in SIL1 KD HeLa cells.
Cell, 2024, 187(14):3652-3670.e40
Autophagy, 2024, 1-22.
Exp Mol Med, 2024, 56(2):408-421.
S8597 LYN-1604 LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
J Virol, 2021, JVI0155021
Exp Eye Res, 2019, 184:126-134
S2924 Laduviglusib (CHIR-99021) HCl Laduviglusib (CHIR-99021; CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.
Nature, 2024, 10.1038/s41586-024-07706-4
Nature, 2024, 632(8027):1073-1081
Cell, 2024, 187(3):692-711.e26
S2215 DAPT DAPT is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.
Nat Biotechnol, 2024, 10.1038/s41587-024-02386-x
Nat Commun, 2024, 15(1):9529
J Clin Invest, 2024, 134(18)e179860
S1241 Vincristine sulfate Vincristine sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.
Nat Commun, 2024, 15(1):4513
Nat Commun, 2024, 15(1):4739
iScience, 2024, 27(1):108667
S7153 10058-F4 10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 promotes a caspase-3-dependent apoptosis and modulates autophagy.
Cell Metab, 2024, S1550-4131(24)00284-5
Cell Stem Cell, 2024, S1934-5909(24)00041-9
Sci Rep, 2024, 14(1):4060
S1274 BX-795 BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively.
EMBO J, 2024, 10.1038/s44318-024-00244-9
PLoS Pathog, 2024, 20(7):e1012170
Vet Microbiol, 2024, 290:109973
S1204 Melatonin Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
Heliyon, 2024, 10(18):e38098
Heliyon, 2024, 10(11):e32571
Zhejiang Da Xue Xue Bao Yi Xue Ban, 2024, 53(4):498-508
S7980 VPS34-IN1 Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy.
EMBO J, 2024, 10.1038/s44318-024-00096-3
bioRxiv, 2024, 10.1101/2024.01.22.575998
Nat Cell Biol, 2023, 25(7):975-988
S3592 4-PBA (4-Phenylbutyric acid) 4-PBA (4-Phenylbutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models.
Int J Biol Sci, 2024, 20(4):1279-1296
Phytomedicine, 2024, 135:156088
J Transl Med, 2024, 22(1):248
S1627 Nitazoxanide Nitazoxanide is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent(IC50 for canine influenza virus ranges from 0.17 to 0.21 μM). Nitazoxanide modulates autophagy and inhibits mTORC1 signaling.
Nat Commun, 2024, 15(1):8708
Mol Ther, 2024, S1525-0016(24)00340-X
Biomed Pharmacother, 2024, 171:116195
S5144 Neferine Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.
Bone Res, 2022, 10(1):27
Cell Death Dis, 2022, 13(11):1000
iScience, 2022, 25(11):105394
S6889 Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
Cell Cycle, 2022, 1-11.
Aging (Albany NY), 2021, 13(13):17097-17117
S1041 STF-62247 STF-62247 is a molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. STF-62247 shows selective toxicity and growth inhibition of renal cells lacking VHL; 25-fold greater sensitivity observed for cells with VHL deficiency compared to wild-type (VHL+).
Neuropsychiatr Dis Treat, 2015, 11:2091-9
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
E3586 Myristica fragrans Extract Myristica Fragrans Extract is extracted from Myristica Fragrans, which has autophagy modulating activity.
E3141 Codonopsis Pilosula Extract Codonopsis Pilosula Extract is obtained from Codonopsis pilosula, exhibits not only an anti-melanogenic effect in normal melanocytes, but also a cytoprotective effect in melanocytes subjected to oxidative stress by inducing autophagy and microphthalmia-associated transcription factor (MITF) expression.
E4692New THZ-P1-2 THZ-P1-2 is an inhibitor of PI5P4K, which covalently binds to cysteines on a disordered loop in PI5P4Kα/β/γ. It inhibits PI5P4Kα kinase activity with an IC50 of 190 nM and disrupts autophagy by impairing autophagosome clearance and increasing TFEB nuclear localization.
E4824New Hydroxychloroquine Hydroxychloroquine (HCQ) is an antimalarial drug that inhibits autophagy and is used to treat systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA). It exhibits immunomodulatory, antithrombotic, and antiplatelet properties. It inhibits the release endothelin-1, a potent vasoconstrictor, and restores impaired angiogenesis in TNF-α-treated endothelial cells in vitro. It also reduces the production of inflammatory cytokines such as TNF-α, IFN-γ, and IL-6 from peripheral blood mononuclear cells, upregulates IL-10 and decreases platelet aggregation.
Cancer Lett, 2024, 596:217009
Int J Mol Sci, 2022, 23(22)14149
E4809New Piperaquine tetraphosphate tetrahydrate Piperaquine tetraphosphate tetrahydrate is an inhibitor of autophagy . It is a bisquinoline antimalarial agent effective against Plasmodium falciparum. Piperaquine tetraphosphate tetrahydrate is useful in antimalarial research.
E4692New THZ-P1-2 THZ-P1-2 is an inhibitor of PI5P4K, which covalently binds to cysteines on a disordered loop in PI5P4Kα/β/γ. It inhibits PI5P4Kα kinase activity with an IC50 of 190 nM and disrupts autophagy by impairing autophagosome clearance and increasing TFEB nuclear localization.

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