EPZ-015666
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Technical Data
Description
EPZ-015666 (GSK3235025) is a potent and selective and orally active PRMT5 inhibitor with a half-maximal inhibitory concentration (IC50) of 22 nM and broad selectivity against a panel of other histone methyltransferases. Treatment of MCL cell lines with EPZ-015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ-015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models. EPZ-015666 represents a validated chemical probe for further study of PRMT5 biology and arginine methylation in cancer and other diseases.