| S1378 |
Ruxolitinib (INCB018424) |
INCB018424 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. |
Pan |
JAK1, IC50: 3.3 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 |
JAK1, IC50: 3.3 nM |
| S2851 |
Baricitinib (LY3009104, INCB028050) |
Baricitinib (LY3009104, INCB028050) 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. Phase 3. |
Pan |
JAK1, IC50: 5.9 nM |
| 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 |
JAK1, IC50: 10 nM |
| S2219 |
Momelotinib (CYT387) |
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3. |
Pan |
JAK1, IC50: 11 nM |
| S7634 |
Cerdulatinib (PRT062070, PRT2070) |
Cerdulatinib (PRT-062070) 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 |
JAK1, IC50: 12 nM |
| S2179 |
LY2784544 |
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 |
JAK1, IC50: 19.8 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 |
JAK1, IC50: 31.63 nM |
| S2789 |
Tofacitinib (CP-690550,Tasocitinib) |
Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1. |
Pan |
JAK1, IC50: 112 nM |
| S5001 |
Tofacitinib (CP-690550) 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. |
Pan |
JAK1, IC50: 112 nM |
| S7036 |
XL019 |
XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1. |
Pan |
JAK1, IC50: 134.3 nM |
| S8057 |
Pacritinib (SB1518) |
Pacritinib (SB1518) 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, respectively. Phase 3. |
Pan |
JAK1, IC50: 1.28 μM |
| S8004 |
ZM 39923 HCl |
ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase. |
Pan |
JAK1, pIC50: 4.4 |
