| S8879 |
Deucravacitinib (BMS-986165) |
Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases. |
Pan |
Tyk2, IC50: 0.02 nM |
| S7634 |
Cerdulatinib (PRT062070) hydrochloride |
Cerdulatinib (PRT-062070, PRT2070) hydrochloride is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
|
Pan |
TYK2, IC50: 0.5 nM |
| S0437 |
SAR-20347 |
SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively. SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling. |
Pan |
TYK2, IC50: 0.6 nM |
| S6789 |
JAK Inhibitor I (Pyridone 6) |
JAK Inhibitor I (Pyridone 6, CMP 6, Compound 6) is a pan-JAK inhibitor with IC50s of 1 nM, 1 nM, 5 nM and 15 nM for JAK2, TYK2, JAK3 and JAK1, respectively. |
Pan |
TYK2, IC50: 1 nM |
| S0374 |
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. |
Pan |
TYK2, Ki: 4.8 nM |
| S1134 |
AT9283 |
AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). |
Pan |
TYK2, IC50: 1 nM-10 nM |
| S2686 |
NVP-BSK805 2HCl |
NVP-BSK805 2HCl is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2. |
Pan |
TYK2, IC50: 10.76 nM |
| S7541 |
Decernotinib (VX-509) |
Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with Ki of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.
|
Pan |
TYK2, Ki: 13 nM |
| S9676 |
Ropsacitinib (PF-06826647) |
Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO). |
Pan |
TYK2, IC50: 17 nM |
| S2902 |
S-Ruxolitinib (INCB018424) |
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. Phase 3. |
Pan |
TYK2, IC50: 19 nM |
| S8804 |
Brepocitinib (PF-06700841) |
Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3. |
Pan |
Tyk2, IC50: 23 nM |
| S7198 |
BIO |
BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells. |
Pan |
TYK2, IC50: 30 nM |
| S2179 |
Gandotinib (LY2784544) |
Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2. |
Pan |
TYK2, IC50: 44 nM |
| S8057 |
Pacritinib |
Pacritinib is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3. |
Pan |
TYK2, IC50: 50 nM |
| S2851 |
Baricitinib |
Baricitinib is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3. |
Pan |
TYK2, IC50: 53 nM |
| S5754 |
Baricitinib phosphate |
Baricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. |
Pan |
TYK2, IC50: 53 nM |
| S8802 |
Delgocitinib (JTE-052) |
Delgocitinib (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. |
Pan |
TYK2, IC50: 58 nM |
| S7144 |
BMS-911543 |
BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2. |
Pan |
TYK2, IC50: 66 nM |
| S8195 |
Oclacitinib maleate |
Oclacitinib maleate (PF-03394197) is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM. It does not inhibit a panel of 38 non-JAK kinases. |
Pan |
TYK2, IC50: 84nM |
| S7605 |
Filgotinib (GLPG0634) |
Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
|
Pan |
TYK2, IC50: 116 nM |
| S8765 |
Abrocitinib (PF-04965842) |
Abrocitinib (PF-04965842) is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively. |
Pan |
TYK2, IC50: 1.253 μM |
| S0384 |
RO495 |
RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). |
Pan |
|
| S5917 |
Solcitinib |
Solcitinib (GLPG0778, GSK2586184) is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively. |
Pan |
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