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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.
M21298 BMS-986202 BMS-986202 is a potent, selective, orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 of 14 μM. BMS-986202 can be used in IL-23-driven echinococcosis BMS-986202 can be used in studies of IL-23-driven echinococcosis, anti-CD40-induced colitis and spontaneous lupus.
M20767 GDC046 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.
M20744 RO495 RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2).
M20695 TG-89 TG-89 is a JAK inhibitor that inhibits JAK2, FLT3, RET and JAK3.
M20288 WYE-175765 WYE-175765 is a JAK3 and YopH inhibitor
M20166 WAY-354189 WAY-354189 is a JAK-STAT inhibitor.
M13853 Itacitinib adipate Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
M13852 Momelotinib sulfate Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
M13851 CHZ868 CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.
M11281 PF-06263276 Pf-06263276 (PF 6263276) is an effective and selective PAN-JAK inhibitor. The IC50 values of JAK1, JAK2, JAK3 and TYK2 were 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM, respectively.
M11253 BD750 BD750 is an effective immunosuppressant of JAK3/STAT5 and inhibits IL-2-induced JAK3/ STAT5-dependent T cell proliferation with IC50 values of 1.5 μM and 1.1 μM in mice and human T cells, respectively.
M11227 FM-479 Fm-479 was a negative control of FM-381 (HY-102046) and showed no activity against JAK3 or other kinases. Fm-381 is a potent covalent reversible inhibitor of JAK3 targeting unique Cys909. For JAK3, FM-381 was 410, 2700 and 3600 times more selective than JAK1, JAK2 and TYK2 with IC50 of 127 pM.
M11186 NVP-BSK805 NVP-BSK805 is a potent, selective, ATP competitive JAK2 inhibitor with an IC50 of 0.5 nM, which is more than 20 times more selective than acting on JAK1, JAK3 and TYK2.
M10837 Izencitinib Izencitinib (TD-1473) is an orally active, nonselective, gut-defined JAK inhibitor. Izencitinib (TD-1473) can be used in ulcerative colitis studies.
M10740 Gusacitinib Gusacitinib (ASN-002) is a potent dual inhibitor of SYK kinase and JAK kinase,IC50 Values are 5-46 nM. Gusacitinib has anti-cancer activity in both solid and hematological tumors.
M10698 FM-381 FM-381 is a potent, covalent, reversible JAK3 inhibitor that targets the Cys909 site. FM-381 for JAK3 IC50 The value is 127 pM, which is 410, 2700, and 3600 times more selective than JAK1, JAK2, and TYK2, respectively.
M10696 Protosappanin A Protosappanin A (PTA), an immune agent, is a major biphenyl compound isolated from Caesalpinia sappan L that inhibits the JAK2/STAT3-dependent inflammatory pathway by down-regulating the phosphorylation of JAK2 and STAT3.
M10474 Delgocitinib (JTE-052) Delgocitinib, also known as LEO-124249 and JTE052, is a potent and selective JAK inhibitor with IC50 values of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
M10437 PF-06700841 PF-06700841 is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. PF-06700841 also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively.
M10417 Delphinidin chloride Delphinidin (chloride) is an anthocyanidin, a natural plant pigment which can modulate JAK/STAT3 and MAPKinase signaling to induce apoptosis in HCT116 cells.



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