JAK1 Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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