GSK3368715-EPZ019997-DataSheet-生命科学试剂-MedChemExpress.pdf

Hotline: 400-820-3792 Inhibitors • Screening Libraries • Proteins www.MedChemE GSK3368715 Cat. No.: HY-128717 CAS No.: 1629013-22-4 Synonyms: EPZ019997 分⼦式: C₂₀H₃₈N₄O₂ 分⼦量: 366.54 作⽤靶点: Histone Methyltransferase 作⽤通路: Epigenetics 储存⽅式: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY ⽣物活性 GSK3368715 (EPZ019997) 是具有⼝服活性的，可逆的，SAM ⾮竞争性 I 型蛋⽩精氨酸甲基转移酶 (PRMTs) 抑 制剂 (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8))。 GSK3368715 (EPZ019997) 导致精氨酸甲基化状态的转变，改变了外显⼦的使⽤，具有很强的抗癌活性 [1]。 IC50 Target 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] 体外研究 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]. 体内研究 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]. 客户使⽤本产品发表的科研⽂献 • Cell Death Dis. 2021 Nov 13;12(11):1080. • Front Pharmacol. 2020 Sep 8;11:569661. • Research Square Print. 26 Oct, 2022 • Univer