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
|
|
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
|
|
S1052 |
Elesclomol (STA-4783)
|
Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand and inhibits FDX1-mediated Fe-S cluster biosynthesis.Elesclomol (STA-4783) is a potent copper ionophore and can be used in the research of copper-dependent cell death (cuproptosis). |
-
J Exp Clin Cancer Res, 2024, 43(1):68
-
Cell Death Dis, 2024, 15(2):149
-
Cell, 2023, 186(11):2361-2379.e25
|
|
S1159 |
Ganetespib (STA-9090)
|
Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3. |
-
Cancer Cell Int, 2024, 24(1):283
-
Front Pharmacol, 2024, 15:1454829
-
Acta Biochim Biophys Sin (Shanghai), 2024, 56(7):1022-1033
|
|
S1142 |
Alvespimycin (17-DMAG) HCl
|
Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. |
-
Nature, 2024, 626(8000):874-880
-
Nature, 2024, 626(8000):874-880
-
Cell, 2024, S0092-8674(24)00583-X
|
|
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
|
|
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
|
|
S3604 |
Triptolide
|
Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway. |
-
J Clin Invest, 2024, 134(15)e171136
-
Clin Transl Med, 2024, 14(2):e1567
-
Cell Rep, 2024, 43(11):114964
|
|
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
|
|
S1175 |
BIIB021
|
BIIB021 (CNF2024) is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2. |
-
EJNMMI Radiopharm Chem, 2024, 9(1):19
-
Cell Rep, 2022, 41(4):111546
-
SLAS Discov, 2022, 27(3):175-184
|
|
S1163 |
Onalespib (AT13387)
|
Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2. |
-
Theranostics, 2024, 14(6):2442-2463
-
Theranostics, 2024, 14(6):2442-2463
-
Nature Communications, 2023, 1221-2023)
|
|
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
|
|
S1498 |
NVP-BEP800
|
NVP-BEP800 (VER82576) is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1. |
-
Blood Cancer J, 2021, 11(3):61
-
Cell Death Dis, 2021, 12(1):114
-
Cell Death Dis, 2021, 12(1):114
|
|
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
|
|
S2639 |
SNX-2112
|
SNX-2112 selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG. |
-
NPJ Breast Cancer, 2022, 8(1):96
-
SLAS Discov, 2022, 27(3):175-184
-
Cell Chem Biol, 2021, S2451-9456(21)00221-X
|
|
S8402 |
KRIBB11
|
KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1). KRIBB11 induces growth arrest and apoptosis. |
-
Mil Med Res, 2024, 11(1):41
-
Nat Commun, 2023, 14(1):6473
-
Nat Commun, 2023, 14(1):6473
|
|
S8299 |
HA15
|
HA15 is a molecule that targets specifically HSPA5 (Heat shock 70kDa protein 5) also known as BiP (Immunoglobulin heavy-chain-binding protein) or Grp78 (glucose-regulated protein 78). HA15 displays anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors. |
-
Clin Transl Med, 2024, 14(2):e1567
-
Cancer Res, 2023, 83(16):2750-2762
-
iScience, 2023, 26(1):105743
|
|
S8039 |
Zelavespib (PU-H71)
|
Zelavespib (PU-H71, NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1. |
-
Breast Cancer Res, 2024, 26(1):33
-
Int J Mol Sci, 2023, 24(14)11585
-
EJNMMI Radiopharm Chem, 2023, 8(1):2
|
|
S7097 |
HSP990 (NVP-HSP990)
|
HSP990 (NVP-HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. NVP-HSP990 induces cell cycle arrest and apoptosis. |
-
EJNMMI Radiopharm Chem, 2024, 9(1):19
-
Virus Res, 2023, 329:199103
-
bioRxiv, 2023, 10.1101/2023.06.15.545197
|
|
S7282 |
NMS-E973
|
NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases. |
-
SLAS Discov, 2022, 27(3):175-184
-
J Exp Clin Cancer Res, 2021, 40(1):170
-
Mol Cancer, 2020, 19(1):112
|
|
S8365 |
Apoptozole
|
Apoptozole (Apoptosis Activator VII) is an inhibitor of heat shock protein 70(HSP70) and Hsc70 with dissociation constants Kd of 0.14 μM and 0.21 μM, respectively. It induces caspase-dependent apoptosis. |
-
Nutrients, 2023, 15(4)992
-
J Virol, 2023, 97(4):e0012823
-
Int J Mol Sci, 2022, 23(23)15229
|
|
S7122 |
XL888
|
XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1. |
-
Cell Commun Signal, 2024, 22(1):428
-
Sci Adv, 2023, 9(35):eade7486
-
SLAS Discov, 2022, 27(3):175-184
|
|
S2656 |
PF-04929113 (SNX-5422)
|
PF-04929113 (SNX-5422) is a potent and selective HSP90 inhibitor with Kd of 41 nM and induces Her-2 degradation with IC50 of 37 nM. Phase 1/2. |
-
ACS Chem Neurosci, 2019, 10(6):2890-2902
-
Endocrine, 2016, 51(2):274-82
-
Antimicrob Agents Chemother, 2014, 58(7):4138-44
|
|
S7750 |
KNK437
|
KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
|
-
Parasit Vectors, 2023, 16(1):168
-
Biosci Rep, 2020, 40(3)
-
Br J Haematol, 2013, 161(5):667-76
|
|
S5006 |
Teprenone
|
Teprenone, an acylic polyisoprenoid, that is known as tetraprenylacetone or geranylgeranylacetone, is an anti-ulcer drug, clinically used for gastritis. Teprenone(Geranylgeranylacetone) is an inducer of heat shock proteins (HSPs) expression. |
-
Inflammopharmacology, 2023, 31(3):1319-1327
-
Antioxidants -Basel, 2022, 11-91741
-
Front Endocrinol (Lausanne), 2021, 12:743202
|
|
S8305 |
TRC051384
|
TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent. |
-
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
-
Front Cell Dev Biol, 2021, 9:796974
-
Mol Cell Biochem, 2021, 10.1007/s11010-021-04052-1
|
|
S7459 |
VER-50589
|
VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
|
-
Antiviral Res, 2023, 211:105553
-
Cell Chem Biol, 2021, S2451-9456(21)00221-X
-
PLoS Negl Trop Dis, 2014, 8(2):e2699
|
|
S7428 |
Rocaglamide
|
Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity. |
-
Life Sci Alliance, 2024, 7(9)e202302396
-
Elife, 2023, 12e69521
-
Blood Adv, 2023, 7(12):2926-2937
|
|
S7458 |
VER-49009
|
VER-49009 (CCT0129397) is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β. |
-
SLAS Discov, 2022, 27(3):175-184
-
Cell Chem Biol, 2021, S2451-9456(21)00221-X
|
|
S7716 |
Pimitespib (TAS-116)
|
Pimitespib (TAS-116) is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L). |
-
Hum Exp Toxicol, 2023, 42:9603271231165678
-
Cancer Res, 2022, CAN-21-3819
|
|
S6721 |
JG98
|
JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. JG-98 induces classical apoptosis features, including morphological changes consistent with programmed cell death and positive annexin staining. JG-98 exhibits anticancer activity. |
-
Cell Commun Signal, 2024, 22(1):217
-
Cell Stress Chaperones, 2024, S1355-8145(24)00072-5
-
FEBS Open Bio, 2023, none
|
|
S2685 |
KW-2478
|
KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1. |
-
Clin Exp Med, 2019, 10.1007/s10238-019-00587-2
|
|
S0279 |
Dimethylenastron
|
Dimethylenastron is a potent, specific and reversible inhibitor of kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) with IC50 of 200 nM. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells. |
-
EMBO Rep, 2023, e57234.
|
|
S9806 |
DTHIB
|
DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities. |
-
Cell Mol Life Sci, 2024, 81(1):386
-
Cancer Sci, 2023, 114(11):4388-4400.
|
|
S0294 |
HSF1A
|
HSF1A is a cell-permeable heat shock transcription factor 1 (HSF1) activator. HSF1A protects cells from stress-induced apoptosis, binds TRiC subunits and inhibits TRiC activity without perturbation of ATP hydrolysis. |
|
|
S6568 |
ML346
|
ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases. |
|
|
E0362 |
BiP Inducer X (BIX)
|
BiP Inducer X (BIX) is a selective GRP78 (BiP, HSPA5) inducer. BIX induces BiP only, in a dose-dependent manner, without induction of other molecules involved in the ER stress response.
|
|
|
E0249 |
Pseudolaric Acid A
|
Pseudolaric acid A, a Hsp90 inhibitor with an IC50 of 0.60 μM, 2.72 μM, 1.36 μM, 2.92 μM and 6.16 μM in HL-60, A549, SMMC-7721, HeLa and SW480 cells respectively, is the main bioactive ingredient in Pseudolarix cortex, and induces cell cycle arrest at G2/M phase and promotes cell death through caspase-8/caspase-3 pathway, demonstrating potent antiproliferation and anticancer activities. |
|
|
S7340 |
CH5138303
|
CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
|
|
|
S6193 |
YUM70
|
YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.Although YUM70 inhibits GRP78 enzymatic activity, it increases the expression of GRP78 by increasing the chaperone translation mechanism. |
|
|
E0701 |
Cucurbitacin D
|
Cucurbitacin D is an active component in Cucurbita texana, disrupts maturation of HSP90 and interactions between Hsp90 and two co-chaperones, Cdc37 and p23. |
|
|
S3404New |
HSP27 inhibitor J2
|
HSP27 inhibitor J2 (J2) is an inhibitor of HSP27, which induces abnormal HSP27 dimers formation and suppresses the generation of HSP27 giant polymers, inhibiting the chaperone role of HSP27 and diminishing its cellular protective function. HSP27 inhibitor J2 (J2) enhances the antiproliferative activity of 17-AAG and increases the sensitivity of cisplatin-induced lung cancer cell growth inhibition. |
|
|
E1208 |
NPX800
|
NPX800 is a potent heat shock factor 1 (HSF1) inhibitor, which has the potential for cancer research. |
|
|
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
|
|
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
|
|
S1159 |
Ganetespib (STA-9090)
|
Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3. |
- Cancer Cell Int, 2024, 24(1):283
- Front Pharmacol, 2024, 15:1454829
- Acta Biochim Biophys Sin (Shanghai), 2024, 56(7):1022-1033
|
|
S1142 |
Alvespimycin (17-DMAG) HCl
|
Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. |
- Nature, 2024, 626(8000):874-880
- Nature, 2024, 626(8000):874-880
- Cell, 2024, S0092-8674(24)00583-X
|
|
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
|
|
S3604 |
Triptolide
|
Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway. |
- J Clin Invest, 2024, 134(15)e171136
- Clin Transl Med, 2024, 14(2):e1567
- Cell Rep, 2024, 43(11):114964
|
|
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
|
|
S1175 |
BIIB021
|
BIIB021 (CNF2024) is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2. |
- EJNMMI Radiopharm Chem, 2024, 9(1):19
- Cell Rep, 2022, 41(4):111546
- SLAS Discov, 2022, 27(3):175-184
|
|
S1163 |
Onalespib (AT13387)
|
Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2. |
- Theranostics, 2024, 14(6):2442-2463
- Theranostics, 2024, 14(6):2442-2463
- Nature Communications, 2023, 1221-2023)
|
|
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
|
|
S1498 |
NVP-BEP800
|
NVP-BEP800 (VER82576) is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1. |
- Blood Cancer J, 2021, 11(3):61
- Cell Death Dis, 2021, 12(1):114
- Cell Death Dis, 2021, 12(1):114
|
|
S2639 |
SNX-2112
|
SNX-2112 selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG. |
- NPJ Breast Cancer, 2022, 8(1):96
- SLAS Discov, 2022, 27(3):175-184
- Cell Chem Biol, 2021, S2451-9456(21)00221-X
|
|
S8402 |
KRIBB11
|
KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1). KRIBB11 induces growth arrest and apoptosis. |
- Mil Med Res, 2024, 11(1):41
- Nat Commun, 2023, 14(1):6473
- Nat Commun, 2023, 14(1):6473
|
|
S8039 |
Zelavespib (PU-H71)
|
Zelavespib (PU-H71, NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1. |
- Breast Cancer Res, 2024, 26(1):33
- Int J Mol Sci, 2023, 24(14)11585
- EJNMMI Radiopharm Chem, 2023, 8(1):2
|
|
S7097 |
HSP990 (NVP-HSP990)
|
HSP990 (NVP-HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. NVP-HSP990 induces cell cycle arrest and apoptosis. |
- EJNMMI Radiopharm Chem, 2024, 9(1):19
- Virus Res, 2023, 329:199103
- bioRxiv, 2023, 10.1101/2023.06.15.545197
|
|
S7282 |
NMS-E973
|
NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases. |
- SLAS Discov, 2022, 27(3):175-184
- J Exp Clin Cancer Res, 2021, 40(1):170
- Mol Cancer, 2020, 19(1):112
|
|
S8365 |
Apoptozole
|
Apoptozole (Apoptosis Activator VII) is an inhibitor of heat shock protein 70(HSP70) and Hsc70 with dissociation constants Kd of 0.14 μM and 0.21 μM, respectively. It induces caspase-dependent apoptosis. |
- Nutrients, 2023, 15(4)992
- J Virol, 2023, 97(4):e0012823
- Int J Mol Sci, 2022, 23(23)15229
|
|
S7122 |
XL888
|
XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1. |
- Cell Commun Signal, 2024, 22(1):428
- Sci Adv, 2023, 9(35):eade7486
- SLAS Discov, 2022, 27(3):175-184
|
|
S2656 |
PF-04929113 (SNX-5422)
|
PF-04929113 (SNX-5422) is a potent and selective HSP90 inhibitor with Kd of 41 nM and induces Her-2 degradation with IC50 of 37 nM. Phase 1/2. |
- ACS Chem Neurosci, 2019, 10(6):2890-2902
- Endocrine, 2016, 51(2):274-82
- Antimicrob Agents Chemother, 2014, 58(7):4138-44
|
|
S7750 |
KNK437
|
KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
|
- Parasit Vectors, 2023, 16(1):168
- Biosci Rep, 2020, 40(3)
- Br J Haematol, 2013, 161(5):667-76
|
|
S7459 |
VER-50589
|
VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
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- Antiviral Res, 2023, 211:105553
- Cell Chem Biol, 2021, S2451-9456(21)00221-X
- PLoS Negl Trop Dis, 2014, 8(2):e2699
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S7428 |
Rocaglamide
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Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity. |
- Life Sci Alliance, 2024, 7(9)e202302396
- Elife, 2023, 12e69521
- Blood Adv, 2023, 7(12):2926-2937
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S7458 |
VER-49009
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VER-49009 (CCT0129397) is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β. |
- SLAS Discov, 2022, 27(3):175-184
- Cell Chem Biol, 2021, S2451-9456(21)00221-X
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S7716 |
Pimitespib (TAS-116)
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Pimitespib (TAS-116) is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L). |
- Hum Exp Toxicol, 2023, 42:9603271231165678
- Cancer Res, 2022, CAN-21-3819
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S6721 |
JG98
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JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. JG-98 induces classical apoptosis features, including morphological changes consistent with programmed cell death and positive annexin staining. JG-98 exhibits anticancer activity. |
- Cell Commun Signal, 2024, 22(1):217
- Cell Stress Chaperones, 2024, S1355-8145(24)00072-5
- FEBS Open Bio, 2023, none
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S2685 |
KW-2478
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KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1. |
- Clin Exp Med, 2019, 10.1007/s10238-019-00587-2
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S9806 |
DTHIB
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DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities. |
- Cell Mol Life Sci, 2024, 81(1):386
- Cancer Sci, 2023, 114(11):4388-4400.
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E0249 |
Pseudolaric Acid A
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Pseudolaric acid A, a Hsp90 inhibitor with an IC50 of 0.60 μM, 2.72 μM, 1.36 μM, 2.92 μM and 6.16 μM in HL-60, A549, SMMC-7721, HeLa and SW480 cells respectively, is the main bioactive ingredient in Pseudolarix cortex, and induces cell cycle arrest at G2/M phase and promotes cell death through caspase-8/caspase-3 pathway, demonstrating potent antiproliferation and anticancer activities. |
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S7340 |
CH5138303
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CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
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S6193 |
YUM70
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YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.Although YUM70 inhibits GRP78 enzymatic activity, it increases the expression of GRP78 by increasing the chaperone translation mechanism. |
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S3404New |
HSP27 inhibitor J2
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HSP27 inhibitor J2 (J2) is an inhibitor of HSP27, which induces abnormal HSP27 dimers formation and suppresses the generation of HSP27 giant polymers, inhibiting the chaperone role of HSP27 and diminishing its cellular protective function. HSP27 inhibitor J2 (J2) enhances the antiproliferative activity of 17-AAG and increases the sensitivity of cisplatin-induced lung cancer cell growth inhibition. |
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E1208 |
NPX800
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NPX800 is a potent heat shock factor 1 (HSF1) inhibitor, which has the potential for cancer research. |
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