GSK3368715 (Synonyms: EPZ019997) |
| Catalog No.GC36191 |
GSK3368715(EPZ019997)는 경구 활성, 가역성, S-아데노실-L-메티오닌(SAM) 비경쟁 유형 I 단백질 아르기닌 메틸트랜스퍼라제(PRMT) 억제제(IC50=3.1 nM(PRMT1), 48 nM(1PRMT3))입니다. PRMT4), 5.7nM(PRMT6), 1.7nM(PRMT8)). GSK3368715(EPZ019997)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.: 1629013-22-4
Sample solution is provided at 25 µL, 10mM.
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GSK3368715 (EPZ019997) 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 (EPZ019997) 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 (EPZ019997) 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 (EPZ019997) 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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