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JAK Janus Kinase

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.
M1787 INCB18424 Ruxolitinib (INCB018424) is a first-in-class, potent, selective JAK1/2 inhibitor with an IC50 of 3.3 nM/2.8 nM. It is more than 130-fold more selective for JAK1, JAK2, and JAK3 than JAK3. It can be used in studies related to pemphigus, myelofibrosis and vitiligo.
M5944 Ruxolitinib phosphate Ruxolitinib phosphate(INCB018424 phosphate) 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.
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.
M2346 Filgotinib Filgotinib (GLPG0634) is the first selective inhibitor of JAK1 and JAK2 with IC50 of 10nM and 28nM respectively.
M2044 AZD1480 AZD1480 is a novel small-molecule inhibitor of JAK1/2 with IC50 of 1.3 nM and 0.26 nM, respectively.
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.
M13851 CHZ868 CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.
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 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.
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.
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 Brepocitinib P-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 (INCB039110) is a potent, selective JAK1 inhibitor with an IC50 value of 2 nM for human JAK1. It has oral bioactivity and potential anti-tumor activity.
M8090 PF-04965842 Abrocitinib is an orally active and selective JAK1 inhibitor with an IC50 value of 29 nM. Abrocitinib reversibly inhibits JAK1 kinase by blocking its ATP-binding site. Abrocitinib (PF-04965842) inhibited TYK2 activity (IC50, 1.253 μM) and phosphorylation of STAT1, STAT3, and STAT5 after stimulation. It can be used in the study of autoimmune diseases.




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