Momelotinib (CYT387): Selectivity & Specificity

Momelotinib (CYT387) is a potent inhibitor of JAK1 JH2-JH1 (143 nM), JAK2 JH2-JH1 (11 nM), JAK3 JH2-JH1 (325 nM), TYK2 JH2-JH1 (252 nM), JAK1 (26.9 nM), JAK2 (1.4 nM), ACVR1 (8.4 nM), hepcidin, STAT6, TSLP, IL-4, IL-5, STAT3, BMP6, BMP2, ALK3, SMAD1, SMAD5, SMAD8, SMAD4, IL-6, JAK, USP6. Momelotinib (CYT387) exhibits the greatest inhibitory potency toward JAK2 (IC50 = 1.4 nM).