GSK3368715 dihydrochloride

Research use only, not for human use.

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8.

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types.

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) significantly effects on the growth of BxPC3 xenografts at all doses tested, reducing tumor growth by 78% and 97% in the 150- and 300-mg/kg dose groups, respectively.

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Others

Other Targets

Histone Methyltransferase

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1628925-77-8

439.46

C20H40Cl2N4O2

>98% (HPLC)

In Vitro:?DMSO : 230 mg/mL (523.37 mM; Ultrasonic ) H2O : 140 mg/mL (318.57 mM; Ultrasonic)

Cl.Cl.CCOCC1(COCC)CCC(CC1)c1n[nH]cc1CN(C)CCNC

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(-20℃)

With Ice Pack

≥ 2 years