CAS: 1802175-06-9

CPI-360 is a drug that inhibits the activity of histone methyltransferases. It is used to treat cancer, as well as other diseases caused by abnormal changes in gene expression. CPI-360 has been shown to inhibit the catalytic subunit of the methyltransferase. In addition to preventing the methylation of histones, it also inhibits transcriptional regulation and nucleosome assembly. An advantage of this drug is that it does not affect normal cellular methylation processes.

CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.