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):2989
-
Acta Neuropathol, 2024, 147(1):28
|
|
S5001 |
Tofacitinib (CP-690550) Citrate
|
Tofacitinib citrate (CP-690550, Tasocitinib) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. Tofacitinib citrate has anti-infection activity. |
-
J Exp Clin Cancer Res, 2024, 43(1):64
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Front Oncol, 2024, 14:1386190
|
|
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
|
|
S2789 |
Tofacitinib
|
Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1. Tofacitinib inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis. |
-
Cell Rep Med, 2024, S2666-3791(23)00615-8
-
Transl Oncol, 2024, 44:101939
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
|
|
S1143 |
AG-490
|
AG-490 is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src. |
-
Cytotherapy, 2024, 26(2):145-156
-
J Neuroinflammation, 2023, 20(1):87
-
iScience, 2023, 26(11):108211
|
|
S2162 |
AZD1480
|
AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1. |
-
J Exp Clin Cancer Res, 2024, 43(1):64
-
Breast Cancer Res, 2024, 26(1):54
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
|
|
S2736 |
Fedratinib (TG101348)
|
Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2. |
-
Cell Rep, 2024, 43(2):113751
-
J Transl Med, 2024, 22(1):369
-
J Transl Med, 2024, 22(1):369
|
|
S2796 |
WP1066
|
WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1. |
-
Nat Commun, 2024, 15(1):1987
-
Cancer Cell Int, 2024, 24(1):60
-
Aging (Albany NY), 2024, 16(4):3554-3582
|
|
S2851 |
Baricitinib
|
Baricitinib is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3. |
-
Cell Mol Life Sci, 2024, 81(1):152
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Sci Rep, 2024, 14(1):4125
|
|
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
|
|
S7605 |
Filgotinib (GLPG0634)
|
Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
|
-
PLoS One, 2024, 19(6):e0297817
-
Inflamm Regen, 2023, 43(1):44
-
Front Immunol, 2023, 14:1087986
|
|
S7119 |
Go6976
|
Go6976 (PD406976) is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
|
-
J Cell Sci, 2023, 136(4)jcs259788
-
Sci Adv, 2023, 9(34):eadi5168
-
Sci Adv, 2023, 9(34):eadi5168
|
|
S7198 |
BIO
|
BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells. |
-
Adv Sci (Weinh), 2023, 10(12):e2206542
-
Bone Res, 2023, 11(1):18
-
J Transl Med, 2023, 21(1):530
|
|
S1134 |
AT9283
|
AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). |
-
J Transl Med, 2024, 22(1):209
-
Int J Mol Sci, 2024, 25(5)2956
-
Sci Rep, 2024, 14(1):8200
|
|
S2902 |
S-Ruxolitinib (INCB018424)
|
S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3. |
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Front Immunol, 2023, 14:1185570
-
Int Immunopharmacol, 2023, 118:109993
|
|
S2179 |
Gandotinib (LY2784544)
|
Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2. |
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
-
Front Immunol, 2022, 13:1001068
|
|
S2692 |
TG101209
|
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET (c-RET) with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations. |
-
Phytomedicine, 2023, 117:154918
-
EBioMedicine, 2022, 78:103963
-
Front Immunol, 2022, 13:1001068
|
|
S7634 |
Cerdulatinib (PRT062070) hydrochloride
|
Cerdulatinib (PRT-062070, PRT2070) hydrochloride is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
|
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Int J Mol Sci, 2023, 24(17)13623
-
Cells, 2023, 12(3)453
|
|
S5754 |
Baricitinib phosphate
|
Baricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. |
-
Cell Mol Life Sci, 2024, 81(1):152
-
J Virol, 2023, 97(12):e0127623
-
Physiol Rep, 2023, 11(19):e15829
|
|
S2686 |
NVP-BSK805 2HCl
|
NVP-BSK805 2HCl is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2. |
-
Int J Mol Sci, 2022, 23(9)4597
-
Sci Rep, 2022, 12(1):7
-
Am J Transplant, 2021, 21(7):2360-2371
|
|
S8057 |
Pacritinib
|
Pacritinib is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3. |
-
Sci Rep, 2024, 14(1):4125
-
J Gen Virol, 2023, 104(5)001858
-
Clin Transl Med, 2022, 12(6):e894
|
|
S2867 |
WHI-P154
|
WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation. |
-
Nat Commun, 2023, 14(1):6908
-
Nat Commun, 2023, 14(1):6908
-
Int J Mol Sci, 2023, 10.3390/ijms241813863
|
|
S7259 |
FLLL32
|
FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. FLLL32 inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
|
-
Cancer Commun -Lond), 2023, 43(10):1117-1142
-
Microbiol Res, 2023, 276:127480
-
Pathol Oncol Res, 2022, 28:1610273
|
|
S2806 |
CEP-33779
|
CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2. |
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
J Transl Med, 2023, 21(1):426
-
Int J Mol Sci, 2022, 23(9)4597
|
|
S7541 |
Decernotinib (VX-509)
|
Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with Ki of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.
|
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Br J Cancer, 2023, 10.1038/s41416-023-02196-z
-
Cells, 2023, 12(5)770
|
|
S8162 |
Upadacitinib
|
Upadacitinib is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1. |
-
Nat Commun, 2024, 15(1):1718
-
Cell Mol Life Sci, 2024, 81(1):152
-
Cell Mol Immunol, 2023, 10.1038/s41423-023-01012-1
|
|
S2214 |
AZ 960
|
AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3. AZ 960 induces apoptosis and growth arrest. |
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Acta Derm Venereol, 2024, 104:adv39950
-
Front Immunol, 2022, 13:1001068
|
|
S8004 |
ZM 39923 HCl
|
ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase. |
-
Sci Rep, 2022, 12(1):7
-
Carcinogenesis, 2020, 41(7):993-1004
-
Int J Biol Sci, 2019, 15(9):1882-1891
|
|
S3566 |
Cerdulatinib (PRT062070)
|
Cerdulatinib (PRT062070, PRT2070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively, also inhibits19 other tested kinases with IC50 less than 200 nM. |
-
NPJ Precis Oncol, 2024, 8(1):74
-
Int J Mol Sci, 2023, 24(17)13623
-
Cells, 2023, 12(9)1295
|
|
S7036 |
XL019
|
XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1. |
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Biochem Pharmacol, 2023, 215:115704
-
Sci Rep, 2022, 12(1):7
|
|
S7144 |
BMS-911543
|
BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2. |
-
Molecules, 2024, 29(8)1801
-
Mol Metab, 2023, 10.1016/j.molmet.2023.101836
-
NPJ Precis Oncol, 2021, 5(1):75
|
|
S2407 |
Curcumol
|
Curcumol is a pure monomer isolated from Rhizoma Curcumaeis with antitumor activities. |
-
J Ethnopharmacol, 2021, 280:114413
-
Cell Prolif, 2020, 53(3):e12762
-
Phytother Res, 2020, 10.1002/ptr.6968
|
|
S5917 |
Solcitinib
|
Solcitinib (GLPG0778, GSK2586184) is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively. |
-
Breast Cancer Res, 2024, 26(1):54
-
Cancer Res, 2023, 83(2):264-284
-
JCI Insight, 2023, 8(22)e164672
|
|
S8195 |
Oclacitinib maleate
|
Oclacitinib maleate (PF-03394197) is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM. It does not inhibit a panel of 38 non-JAK kinases. |
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Molecules, 2024, 29(8)1801
-
Sci Rep, 2022, 12(1):7
|
|
S6789 |
Pyridone 6
|
Pyridone 6 is a pan-JAK inhibitor with IC50s of 1 nM, 1 nM, 5 nM and 15 nM for JAK2, TYK2, JAK3 and JAK1, respectively. |
-
Mol Metab, 2023, 10.1016/j.molmet.2023.101836
-
Nat Commun, 2022, 13(1):6226
-
Nat Commun, 2022, 13(1):6226
|
|
S8765 |
Abrocitinib (PF-04965842)
|
Abrocitinib (PF-04965842) is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively. |
-
Molecules, 2024, 29(8)1801
-
Acta Derm Venereol, 2024, 104:adv39950
-
Cells, 2022, 11(22)3588
|
|
S5588 |
Creatine
|
Creatine (Methylguanidoacetic acid) is a nitrogenous organic acid that occurs naturally in vertebrates. It facilitates the recycling of adenosine triphosphate (ATP) primarily in muscle and brain tissue.Creatine can inhibits the JAK-STAT1 signal transmission by inhibiting the interaction of IFN-γ receptors with JAK2 in an ATP-independent manner, thereby inhibiting downstream pro-inflammatory gene expression. |
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Aging (Albany NY), 2022, 14(16):6796-6808
-
Cancer Cell, 2021, S1535-6108(21)00445-1
-
Histochem Cell Biol, 2021, 156(3):227-237
|
|
S8538 |
Ritlecitinib (PF-06651600)
|
Ritlecitinib (PF-06651600) is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2. |
-
Molecules, 2024, 29(8)1801
-
Drug Des Devel Ther, 2022, 16:363-374
-
Front Oncol, 2021, 11:807200
|
|
S8879 |
Deucravacitinib (BMS-986165)
|
Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases. |
-
Nat Commun, 2024, 15(1):1718
-
Nat Commun, 2024, 15(1):1337
-
Front Immunol, 2023, 10.3389/fimmu.2023.1263926
|
|
S7812 |
Itacitinib (INCB39110)
|
Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity. |
-
Molecules, 2024, 29(8)1801
-
J Physiol, 2023, 10.1113/JP284393
-
Nat Chem Biol, 2022, 10.1038/s41589-022-01098-0
|
|
S7650 |
Peficitinib
|
Peficitinib is an orally bioavailable JAK inhibitor. Phase 3.
|
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Int Immunopharmacol, 2023, 122:110630
|
|
S0981 |
BD750
|
BD750 is an immunosuppressant and a dual inhibitor of JAK3 and STAT5 that inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation with IC50 of 1.5 μM and 1.1 μM for mouse and human T-cell proliferation, respectively. |
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Bioengineered, 2022, 13(6):14616-14631
|
|
S5904 |
WHI-P97
|
WHI-P97 is a potent inhibitor of JAK-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays. |
-
J Med Chem, 2020, 31
|
|
S5903 |
JANEX-1
|
JANEX-1 (WHI-P131) is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 at an IC50 of 78 µM without altering the activity of JAK1 or JAK2, or any other protein tyrosine kinases (IC50 ≥ 350 µM). |
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J Cell Commun Signal, 2024, 18(1):e12017
-
JCI Insight, 2023, 8(22)e164672
-
Exp Biol Med (Maywood), 2020, 1535370220942470
|
|
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
|
|
S5902 |
1,2,3,4,5,6-Hexabromocyclohexane
|
1,2,3,4,5,6-Hexabromocyclohexane (NSC7908) is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation with IC50 value to be estimated in low micromolar range. |
-
Cell Tissue Res, 2016, 364(2):395-404
|
|
S8804 |
Brepocitinib (PF-06700841)
|
Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3. |
-
Cancer Immunol Res, 2021, 9-5:542-553
|
|
S8541 |
FM-381
|
FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively. |
-
Commun Biol, 2020, 3:8
|
|
S0437 |
SAR-20347
|
SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively. SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling. |
-
Cancer Discov, 2023, 13(2):410-431
-
Cancer Discov, 2023, 13(2):410-431
|
|
S8684 |
Selective JAK3 inhibitor 1
|
Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK. |
-
Cancer Sci, 2023, 114(6):2622-2633
|
|
S6899 |
Licochalcone D
|
Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. |
|
|
S6521 |
WHI-P258
|
WHI-P258 is an inhibitor of JAK3 with Ki value of 72 μM. |
|
|
S0918 |
Ginkgolic acid C17:1
|
Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells. |
|
|
S7002 |
Zotiraciclib
|
Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency. |
|
|
E1526New |
Zasocitinib
|
Zasocitinib( NDI-034858, TAK-279) is a TYK2 inhibitor, which is currently being investigated in a phase IIb trial for moderate-to-severe plaque psoriasis. |
|
|
S3267 |
Nicotiflorin (Kaempferol-3-O-rutinoside)
|
Nicotiflorin (Kaempferol-3-O-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity. |
|
|
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. |
|
|
S6524 |
NSC 42834
|
NSC42834 (JAK2 Inhibitor V, Z3) is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2 with IC50 values between 10 and 30 μM. |
|
|
E0011 |
Linderalactone
|
Linderalactone inhibits human lung cancer growth by modulating the expression of apoptosis-related proteins (Bax and Bcl-2) with an IC50 of 15 µM in A-549 cells. Linderalactone induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. Linderalactone can be isolated from Radix linderae. |
|
|
S0871 |
Gusacitinib (ASN-002)
|
Gusacitinib (ASN-002) is a novel and potent dual inhibitor of spleen tyrosine kinase (SYK) and Janus kinases (JAK) with IC50 values of 5-46 nM in biochemical assays. |
|
|
E2821 |
RGB-286638 free base
|
RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM. |
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E0793 |
G5-7
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G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. |
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E0769 |
Ginsenoside Rh4
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Ginsenoside Rh4 is an important active ingredient of traditional Chinese medicine ginseng, which has been shown to inhibit Wnt/β-Catenin, JAK2/STAT3, TGF-β/Smad2/3 and other signaling pathways. |
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S0374 |
GDC046
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GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively. |
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S7137 |
GLPG0634 analogue
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GLPG0634 analogue is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
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S0384 |
RO495
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RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). |
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S1349 |
SC99
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SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway by docking into the ATP-binding pocket of JAK2, also inhibits phosphorylation of JAK2and STAT3 with no effects on the other kinases associated with STAT3 signaling. |
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S0391 |
TG-89
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TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM. |
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S8802 |
Delgocitinib (JTE-052)
|
Delgocitinib (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. |
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E0700 |
cucurbitacin E
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Cucurbitacin E (α-Elaterin; α-Elaterine), a tetracyclic triterpene derived from the climbing stem of Cucumic melo L, is an inhibitor of JAK2 and STAT3. |
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S9676 |
Ropsacitinib (PF-06826647)
|
Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO). |
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S8152 |
Cucurbitacin I
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Cucurbitacin-I (Elatericin B, JSI 124, NSC 521777), a natural cell-permeable triterpenoid isolated from Cucurbitaceae, is a novel selective inhibitor of JAK2/STAT3.
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E1435New |
Tinengotinib
|
Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC). |
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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):2989
- Acta Neuropathol, 2024, 147(1):28
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S5001 |
Tofacitinib (CP-690550) Citrate
|
Tofacitinib citrate (CP-690550, Tasocitinib) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. Tofacitinib citrate has anti-infection activity. |
- J Exp Clin Cancer Res, 2024, 43(1):64
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Front Oncol, 2024, 14:1386190
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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
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S2789 |
Tofacitinib
|
Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1. Tofacitinib inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis. |
- Cell Rep Med, 2024, S2666-3791(23)00615-8
- Transl Oncol, 2024, 44:101939
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
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S1143 |
AG-490
|
AG-490 is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src. |
- Cytotherapy, 2024, 26(2):145-156
- J Neuroinflammation, 2023, 20(1):87
- iScience, 2023, 26(11):108211
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S2162 |
AZD1480
|
AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1. |
- J Exp Clin Cancer Res, 2024, 43(1):64
- Breast Cancer Res, 2024, 26(1):54
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
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S2736 |
Fedratinib (TG101348)
|
Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2. |
- Cell Rep, 2024, 43(2):113751
- J Transl Med, 2024, 22(1):369
- J Transl Med, 2024, 22(1):369
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S2796 |
WP1066
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WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1. |
- Nat Commun, 2024, 15(1):1987
- Cancer Cell Int, 2024, 24(1):60
- Aging (Albany NY), 2024, 16(4):3554-3582
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S2851 |
Baricitinib
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Baricitinib is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3. |
- Cell Mol Life Sci, 2024, 81(1):152
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Sci Rep, 2024, 14(1):4125
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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
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S7605 |
Filgotinib (GLPG0634)
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Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
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- PLoS One, 2024, 19(6):e0297817
- Inflamm Regen, 2023, 43(1):44
- Front Immunol, 2023, 14:1087986
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S7119 |
Go6976
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Go6976 (PD406976) is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
|
- J Cell Sci, 2023, 136(4)jcs259788
- Sci Adv, 2023, 9(34):eadi5168
- Sci Adv, 2023, 9(34):eadi5168
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S7198 |
BIO
|
BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells. |
- Adv Sci (Weinh), 2023, 10(12):e2206542
- Bone Res, 2023, 11(1):18
- J Transl Med, 2023, 21(1):530
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S1134 |
AT9283
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AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). |
- J Transl Med, 2024, 22(1):209
- Int J Mol Sci, 2024, 25(5)2956
- Sci Rep, 2024, 14(1):8200
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S2902 |
S-Ruxolitinib (INCB018424)
|
S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3. |
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Front Immunol, 2023, 14:1185570
- Int Immunopharmacol, 2023, 118:109993
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S2179 |
Gandotinib (LY2784544)
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Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2. |
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
- Front Immunol, 2022, 13:1001068
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S2692 |
TG101209
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TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET (c-RET) with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations. |
- Phytomedicine, 2023, 117:154918
- EBioMedicine, 2022, 78:103963
- Front Immunol, 2022, 13:1001068
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S7634 |
Cerdulatinib (PRT062070) hydrochloride
|
Cerdulatinib (PRT-062070, PRT2070) hydrochloride is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
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- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Int J Mol Sci, 2023, 24(17)13623
- Cells, 2023, 12(3)453
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S5754 |
Baricitinib phosphate
|
Baricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. |
- Cell Mol Life Sci, 2024, 81(1):152
- J Virol, 2023, 97(12):e0127623
- Physiol Rep, 2023, 11(19):e15829
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S2686 |
NVP-BSK805 2HCl
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NVP-BSK805 2HCl is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2. |
- Int J Mol Sci, 2022, 23(9)4597
- Sci Rep, 2022, 12(1):7
- Am J Transplant, 2021, 21(7):2360-2371
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S8057 |
Pacritinib
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Pacritinib is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3. |
- Sci Rep, 2024, 14(1):4125
- J Gen Virol, 2023, 104(5)001858
- Clin Transl Med, 2022, 12(6):e894
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S2867 |
WHI-P154
|
WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation. |
- Nat Commun, 2023, 14(1):6908
- Nat Commun, 2023, 14(1):6908
- Int J Mol Sci, 2023, 10.3390/ijms241813863
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S7259 |
FLLL32
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FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. FLLL32 inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
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- Cancer Commun -Lond), 2023, 43(10):1117-1142
- Microbiol Res, 2023, 276:127480
- Pathol Oncol Res, 2022, 28:1610273
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S2806 |
CEP-33779
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CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2. |
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- J Transl Med, 2023, 21(1):426
- Int J Mol Sci, 2022, 23(9)4597
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S7541 |
Decernotinib (VX-509)
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Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with Ki of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.
|
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Br J Cancer, 2023, 10.1038/s41416-023-02196-z
- Cells, 2023, 12(5)770
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S8162 |
Upadacitinib
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Upadacitinib is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1. |
- Nat Commun, 2024, 15(1):1718
- Cell Mol Life Sci, 2024, 81(1):152
- Cell Mol Immunol, 2023, 10.1038/s41423-023-01012-1
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S2214 |
AZ 960
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AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3. AZ 960 induces apoptosis and growth arrest. |
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Acta Derm Venereol, 2024, 104:adv39950
- Front Immunol, 2022, 13:1001068
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S8004 |
ZM 39923 HCl
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ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase. |
- Sci Rep, 2022, 12(1):7
- Carcinogenesis, 2020, 41(7):993-1004
- Int J Biol Sci, 2019, 15(9):1882-1891
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S3566 |
Cerdulatinib (PRT062070)
|
Cerdulatinib (PRT062070, PRT2070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively, also inhibits19 other tested kinases with IC50 less than 200 nM. |
- NPJ Precis Oncol, 2024, 8(1):74
- Int J Mol Sci, 2023, 24(17)13623
- Cells, 2023, 12(9)1295
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S7036 |
XL019
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XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1. |
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Biochem Pharmacol, 2023, 215:115704
- Sci Rep, 2022, 12(1):7
|
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S7144 |
BMS-911543
|
BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2. |
- Molecules, 2024, 29(8)1801
- Mol Metab, 2023, 10.1016/j.molmet.2023.101836
- NPJ Precis Oncol, 2021, 5(1):75
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S2407 |
Curcumol
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Curcumol is a pure monomer isolated from Rhizoma Curcumaeis with antitumor activities. |
- J Ethnopharmacol, 2021, 280:114413
- Cell Prolif, 2020, 53(3):e12762
- Phytother Res, 2020, 10.1002/ptr.6968
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S5917 |
Solcitinib
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Solcitinib (GLPG0778, GSK2586184) is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively. |
- Breast Cancer Res, 2024, 26(1):54
- Cancer Res, 2023, 83(2):264-284
- JCI Insight, 2023, 8(22)e164672
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S8195 |
Oclacitinib maleate
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Oclacitinib maleate (PF-03394197) is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM. It does not inhibit a panel of 38 non-JAK kinases. |
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Molecules, 2024, 29(8)1801
- Sci Rep, 2022, 12(1):7
|
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S6789 |
Pyridone 6
|
Pyridone 6 is a pan-JAK inhibitor with IC50s of 1 nM, 1 nM, 5 nM and 15 nM for JAK2, TYK2, JAK3 and JAK1, respectively. |
- Mol Metab, 2023, 10.1016/j.molmet.2023.101836
- Nat Commun, 2022, 13(1):6226
- Nat Commun, 2022, 13(1):6226
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S8765 |
Abrocitinib (PF-04965842)
|
Abrocitinib (PF-04965842) is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively. |
- Molecules, 2024, 29(8)1801
- Acta Derm Venereol, 2024, 104:adv39950
- Cells, 2022, 11(22)3588
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S5588 |
Creatine
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Creatine (Methylguanidoacetic acid) is a nitrogenous organic acid that occurs naturally in vertebrates. It facilitates the recycling of adenosine triphosphate (ATP) primarily in muscle and brain tissue.Creatine can inhibits the JAK-STAT1 signal transmission by inhibiting the interaction of IFN-γ receptors with JAK2 in an ATP-independent manner, thereby inhibiting downstream pro-inflammatory gene expression. |
- Aging (Albany NY), 2022, 14(16):6796-6808
- Cancer Cell, 2021, S1535-6108(21)00445-1
- Histochem Cell Biol, 2021, 156(3):227-237
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S8538 |
Ritlecitinib (PF-06651600)
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Ritlecitinib (PF-06651600) is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2. |
- Molecules, 2024, 29(8)1801
- Drug Des Devel Ther, 2022, 16:363-374
- Front Oncol, 2021, 11:807200
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S8879 |
Deucravacitinib (BMS-986165)
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Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases. |
- Nat Commun, 2024, 15(1):1718
- Nat Commun, 2024, 15(1):1337
- Front Immunol, 2023, 10.3389/fimmu.2023.1263926
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S7812 |
Itacitinib (INCB39110)
|
Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity. |
- Molecules, 2024, 29(8)1801
- J Physiol, 2023, 10.1113/JP284393
- Nat Chem Biol, 2022, 10.1038/s41589-022-01098-0
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S7650 |
Peficitinib
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Peficitinib is an orally bioavailable JAK inhibitor. Phase 3.
|
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Int Immunopharmacol, 2023, 122:110630
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S0981 |
BD750
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BD750 is an immunosuppressant and a dual inhibitor of JAK3 and STAT5 that inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation with IC50 of 1.5 μM and 1.1 μM for mouse and human T-cell proliferation, respectively. |
- Bioengineered, 2022, 13(6):14616-14631
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S5904 |
WHI-P97
|
WHI-P97 is a potent inhibitor of JAK-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays. |
- J Med Chem, 2020, 31
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S5903 |
JANEX-1
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JANEX-1 (WHI-P131) is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 at an IC50 of 78 µM without altering the activity of JAK1 or JAK2, or any other protein tyrosine kinases (IC50 ≥ 350 µM). |
- J Cell Commun Signal, 2024, 18(1):e12017
- JCI Insight, 2023, 8(22)e164672
- Exp Biol Med (Maywood), 2020, 1535370220942470
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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
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S5902 |
1,2,3,4,5,6-Hexabromocyclohexane
|
1,2,3,4,5,6-Hexabromocyclohexane (NSC7908) is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation with IC50 value to be estimated in low micromolar range. |
- Cell Tissue Res, 2016, 364(2):395-404
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S8804 |
Brepocitinib (PF-06700841)
|
Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3. |
- Cancer Immunol Res, 2021, 9-5:542-553
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S8541 |
FM-381
|
FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively. |
- Commun Biol, 2020, 3:8
|
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S0437 |
SAR-20347
|
SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively. SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling. |
- Cancer Discov, 2023, 13(2):410-431
- Cancer Discov, 2023, 13(2):410-431
|
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S8684 |
Selective JAK3 inhibitor 1
|
Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK. |
- Cancer Sci, 2023, 114(6):2622-2633
|
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S6899 |
Licochalcone D
|
Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. |
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S6521 |
WHI-P258
|
WHI-P258 is an inhibitor of JAK3 with Ki value of 72 μM. |
|
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S0918 |
Ginkgolic acid C17:1
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Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells. |
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S7002 |
Zotiraciclib
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Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency. |
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E1526New |
Zasocitinib
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Zasocitinib( NDI-034858, TAK-279) is a TYK2 inhibitor, which is currently being investigated in a phase IIb trial for moderate-to-severe plaque psoriasis. |
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S3267 |
Nicotiflorin (Kaempferol-3-O-rutinoside)
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Nicotiflorin (Kaempferol-3-O-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity. |
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S5554 |
Lanatoside C
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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. |
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S6524 |
NSC 42834
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NSC42834 (JAK2 Inhibitor V, Z3) is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2 with IC50 values between 10 and 30 μM. |
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E0011 |
Linderalactone
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Linderalactone inhibits human lung cancer growth by modulating the expression of apoptosis-related proteins (Bax and Bcl-2) with an IC50 of 15 µM in A-549 cells. Linderalactone induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. Linderalactone can be isolated from Radix linderae. |
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S0871 |
Gusacitinib (ASN-002)
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Gusacitinib (ASN-002) is a novel and potent dual inhibitor of spleen tyrosine kinase (SYK) and Janus kinases (JAK) with IC50 values of 5-46 nM in biochemical assays. |
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E2821 |
RGB-286638 free base
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RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM. |
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E0793 |
G5-7
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G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. |
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E0769 |
Ginsenoside Rh4
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Ginsenoside Rh4 is an important active ingredient of traditional Chinese medicine ginseng, which has been shown to inhibit Wnt/β-Catenin, JAK2/STAT3, TGF-β/Smad2/3 and other signaling pathways. |
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S0374 |
GDC046
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GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively. |
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S7137 |
GLPG0634 analogue
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GLPG0634 analogue is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
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S0384 |
RO495
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RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). |
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S1349 |
SC99
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SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway by docking into the ATP-binding pocket of JAK2, also inhibits phosphorylation of JAK2and STAT3 with no effects on the other kinases associated with STAT3 signaling. |
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S0391 |
TG-89
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TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM. |
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S8802 |
Delgocitinib (JTE-052)
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Delgocitinib (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. |
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E0700 |
cucurbitacin E
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Cucurbitacin E (α-Elaterin; α-Elaterine), a tetracyclic triterpene derived from the climbing stem of Cucumic melo L, is an inhibitor of JAK2 and STAT3. |
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S9676 |
Ropsacitinib (PF-06826647)
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Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO). |
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S8152 |
Cucurbitacin I
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Cucurbitacin-I (Elatericin B, JSI 124, NSC 521777), a natural cell-permeable triterpenoid isolated from Cucurbitaceae, is a novel selective inhibitor of JAK2/STAT3.
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E1435New |
Tinengotinib
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Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC). |
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