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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