gsk-3368715

GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.

GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 是一种具有口服活性和高效性的 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂 ，具有抗癌和抗肿瘤活性，抑制PRMT1，PRMT3，PRMT4，PRMT6，PRMT8的活性，可用于研究晚期实体肿瘤。

GSK3368715, a first-in-class, orally active, potent, and selective SAM-noncompetitive inhibitor of Type I Protein Arginine Methyltransferases (PRMTs), exhibits anti-tumor efficacy across multiple cancer models and alters exon usage with IC50 values in the lower nM range. It synergizes with GSK3326595 (Type II inhibitor) (Axon 3750) to inhibit tumor growth.