GSK3368715 dihydrochloride (Synonyms: EPZ019997 dihydrochloride) |
| Catalog No.GC36192 |
GSK3368715 디히드로클로라이드(EPZ019997 디히드로클로라이드)는 경구 활성, 가역적, S-아데노실-L-메티오닌(SAM) 비경쟁적 유형 I 단백질 아르기닌 메틸트랜스퍼라제(PRMT) 억제제(IC50=3.1nM(PRMT3)nM(PRMT3), 148)입니다. nM(PRMT4), 5.7nM(PRMT6), 1.7nM(PRMT8)). GSK3368715 디히드로클로라이드(EPZ019997 디히드로클로라이드)는 아르기닌 메틸화 상태의 이동을 생성하고 엑손 사용을 변경하며 강력한 항암 활성을 가지고 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1628925-77-8
Sample solution is provided at 25 µL, 10mM.
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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[1]. IC50: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)[1]Kiapp: 1.5 nM (PRMT1), 81 nM (PRMT3), 19 nM (PRMT4), 2.4 nM (PRMT6), 2 nM (PRMT8)[1]
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[1].
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[1].
[1]. Fedoriw A, et al. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss. Cancer Cell. 2019 Jul 8;36(1):100-114.e25.
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