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JAK Janus Kinase

Inhibitors

Cat.No.  Name Information
M3030 S-Ruxolitinib 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.
M1820 Tofacitinib Tofacitinib (formerly tasocitinib, CP-690550) is a novel Janus Kinase 3 (JAK-3) kinase inhibitor with an IC50 value estimated at 0.2 μM.
M1660 AZ 960 AZ 960 is a novel and specific inhibitor of the JAK2 kinase with a Ki of 0.45nM in vitro.
M1646 AG490 AG490 (Tyrphostin AG490) is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively).
M1733 TG101348 TG101348 is a selective small-molecule Janus kinase 2 (JAK2) inhibitor with IC50 of 3 nM.
M4670 Curculigoside Curculigoside is the main saponin in C. orchioide, which has significant antioxidant, anti-osteoporosis, anti-depression and neuroprotective effects. By regulating the JAK/STAT/NF-κB signaling pathway, it showed significant anti-arthritis effects in vivo and in vitro.
M4138 Deucravacitinib (BMS-986165) Deucravacitinib (BMS-986165) is a first-in-class, selective, orally bioavailable inhibitor of TYK2 transitions.Deucravacitinib selectively binds the TYK2 pseudokinase (JH2) structural domain with an IC50 of 1.0 nM and a Ki value of 0.02 nM. Deucravacitinib (BMS-986165) blocks receptor-mediated Tyk2 activation by stably regulating the JH2 structural domain. deucravacitinib also inhibits the IL-12/23 and type I IFN pathways. deucravacitinib may be used in psoriasis research.
M3801 TCS 21311 TCS 21311 is a potent JAK3 inhibitor with IC50 of 8 nM.
M3737 Pyridone 6 Pyridone 6 is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK1 (IC50 = 15 nM for murine JAK1), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk 2 (IC50 = 1 nM) (Janus protein tyrosine kinases).
M3735 JAK2 Inhibitor V JAK2 Inhibitor V, Z3 is a novel specific inhibitor of Jak2 which inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
M3616 Tofacitinib citrate Tofacitinib (CP-690550) Citrate is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.
M3535 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.
M3141 ZM 39923 hydrochloride ZM 39923 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.
M3130 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.
M3030 S-Ruxolitinib 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.
M2912 Pacritinib Pacritinib (SB1518) is an effective mutant inhibitor of wild-type JAK2 and JAK2V617F with IC50 of 23 nM and 19 nM, respectively. Pacritinib also inhibited FLT3 and its mutant FLT3D835Y with IC50 of 22 nM and 6 nM, respectively.
M2566 XL019 XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2.
M2466 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.
M2346 Filgotinib Filgotinib (GLPG0634) is the first selective inhibitor of JAK1 and JAK2 with IC50 of 10nM and 28nM respectively.
M2125 WP1066 WP1066 is a potent, novel inhibitor of JAK2 and STAT3 with IC50 of 2.3 μM and 2.43 μM in HEL cells.
M2064 CEP-33779 CEP-33779 is a novel, orally active, selective JAK2 inhibitor with IC50 of 1.8 nM.
M2044 AZD1480 AZD1480 is a novel small-molecule inhibitor of JAK1/2 with IC50 of 1.3 nM and 0.26 nM, respectively.
M2039 Baricitinib Baricitinib (INCB28050) is an oral JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
M1887 TG101209 TG101209 is a novel small molecule, ATP-competitive JAK2-selective kinase inhibitor (IC50 = 6 nM).
M1820 Tofacitinib Tofacitinib (formerly tasocitinib, CP-690550) is a novel Janus Kinase 3 (JAK-3) kinase inhibitor with an IC50 value estimated at 0.2 μM.



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