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 first-in-class oral dual inhibitor of JAK1 and TYK2 with IC50 values 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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