Pricing updated 2019-04-24. Prices are subject to change without notice.
EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6; IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively).1 It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50 = 0.637 µM).1 EPZ020411 shows a moderate clearance rate in rats following intravenous bolus administration, and, following 5 mg/kg subcutaneous dosing, has an unbound blood concentration exceeding the PRMT6 biochemical IC50 value for more than 12 hours.1
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1. Mitchell, L.H., Drew, A.E., Ribich, S.A., et al. Aryl pyrazoles as potent inhibitors of arginine methyltransferases: Identification of the first PRMT6 tool compound ACS Med. Chem. Lett. 6, 655-659 (2015).