CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM[1]. Chk1|0.4 nM (IC50)
CHK1-IN-3 effectively inhibites the growth of malignant hematopathy cell lines especially Z-138 (IC50: 0.013 µM) and displays low affinity for hERG (IC50 > 40 µM)[1].
CHK1-IN-3 significantly suppresses the tumor growth in Z-138 cell inoculated xenograft model as a single agent with body weight unaffected[1].
[1]. Tong L, et al. Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies. Eur J Med Chem. 2019 Jul 1;173:44-62.