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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.
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 dihydrochloride NVP-BSK805 2HCl 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.
M10377 Golidocitinib (AZD4205) Golidocitinib (AZD4205) is a novel potent and selective janus kinase 1 (JAK1) inhibitor, with IC50 value of 73 nM.
M9930 PF-06826647 PF-06826647, also known as Tyk2-IN-8, is a selective and orally administered tyrosine kinase 2 (TYK2) inhibitor, with IC50 of 17 nM.
M9853 PF-06700841 tosylate PF-06700841 (Brepocitinib) tosylate is a dual inhibitor of JAK1 and TYK2, with IC50 values of 17 nM and 23 nM, respectively.
M9627 JAK3-IN-6 (Compound 2) JAK3-IN-6 (Compound 2) CAS#: 1443235-95-7 is a potent and highly selective JAK3 inhibitor, with an IC50 of 0.15 nM.
M9147 Peficitinib Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
M9142 FLLL32 FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.
M9035 WHI-P97 WHI-P97 is a JAK3 inhibitor with an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays.
M8996 SAR-20347 SAR-20347 is a potent dual inhibitor of JAK1 and TYK2 with IC50 values of 23 and 0.6 nM, respectively.
M8876 Itacitinib Itacitinib, also known as INCB39110 or INCB039110, is a potent JAK1 tyrosine kinase inhibitor.



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