ZT55

ZT55 (JAK inhibitor ZT55) is a novel potent, highly-selective tyrosine kinase JAK2 inhibitor with IC50 of 31 nM; displays no significant activity against JAK1/3 (IC50>10 uM); exhibits potent effects on the cellular JAK-STAT pathway, inhibiting tyrosine phosphorylation in JAK2V617F and downstream STAT3/5 transcription factors; inhibits the proliferation of the JAK2V617F-expressing HEL cell line, leading to cell cycle arrest at the G2/M phase and induction of caspase-dependent apoptosis; significantly suppressed the growth of HEL xenograft tumors in vivo, blocks erythroid colony formation of peripheral blood hematopoietic progenitors from patients carrying the JAK2V617F mutation.

References 1. Hu M, et al. J Exp Clin Cancer Res. 2019 Feb 4;38(1):49. View Related Products by Target JAK