GSK-3685032-DataSheet-生命科学试剂-MedChemExpress.pdf

Hotline: 400-820-3792 Inhibitors • Screening Libraries • Proteins www.MedChemE GSK-3685032 Cat. No.: HY-139664 CAS No.: 2170137-61-6 分⼦式: C₂₂H₂₄N₆OS 分⼦量: 420.53 作⽤靶点: DNA Methyltransferase 作⽤通路: Epigenetics 储存⽅式: Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month BIOLOGICAL ACTIVITY ⽣物活性 GSK-3685032 是⼀种⾮时间依赖、⾮共价、可逆的 DNMT1 选择性抑制剂，IC50=0.036 μM。GSK-3685032 诱导 DNA 甲基化丧失、转录激活和癌细胞⽣长抑制 [1]。 IC50 Target DNMT1 [1] 体外研究 GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM [1]. GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course [1]. GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription [1]. GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression [1]. GSK3685032 induces DNA hypomethylation and gene activation [1]. Cell Proliferation Assay [1] Cell Line: 15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR ce