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Description
A xanthenyl compound that inhibits the activities of protein arginine methyltransferases (PRMT) Hmt1p, PRMT1/3/4/6 (IC50 against yeast Hmt1p & human PRMT1 = 0.78 & 1.41 µ,M, respectively), as well as histone lysine methyltransferases (HMTases) SET7 and DOT1 in an AdoMet/SAM- (S-adenosylmethionine) competitive manner. Although SAM-competitive inhibitors generally exhibit broad activity against and are non-selective toward most SAM-utilizing enzymes, AMI-5 is known to be inactive against at least two HMTases (Suv39H1 & Suv39H2).
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