EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has 10 fold selectivity for PRMT6 over PRMT1 and PRMT8. IC50 value: 10 nM Target: PRMT6 in vitro: EPZ020411 inhibits methylation of PRMT6 substrates in cells. EPZ020411 does-dependently inhibits H3R2 methylation in PRMT6-overexpressing cells. in vivo: EPZ020411 shows good bioavailability following subcutaneous (SC) dosing in rats making it a suitable tool for in vivo studies.
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