CHR-6494 TFA is a potent haspin inhibitor with an IC50 of 2 nM, inhibiting histone H3T3 phosphorylation. It induces apoptosis in cancer cells, including melanoma and breast cancer, and is useful for cancer research.

Haspin:2 nM (IC50)

Administration of CHR-6494 (TFA; 0-10-5?nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with an IC50s of 500?nM, 473?nM, 752?nM and 1059 nM, respectively[1]. Administration of CHR-6494 (TFA; 500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification, and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1[1].

Administration of CHR-6494 (TFA; 50?mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor and no obvious body weight change is observed in nude mice bearing HCT-116 human colorectal cancer cells[1].