化合物GSK591 T6853

Product Introduction
Bioactivity


英文名: GSK591

描述: GSK591 (GSK3203591) 是一种有效的精氨酸甲基转移酶 PRMT5 选择性抑制剂，IC50值为 11 nM。

激酶实验: Selectivity profiling experiments: The lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or GSK2141795) on an end-over-end shaker for 45 min at 4 °C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4 °C, for both qualitative and quantitative experiments. The beads are washed with 1× CP buffer and collected by centrifugation. Bound proteins are eluted with 2× NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide.

体外活性: In an in vitro biochemical assay, GSK591 potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4 with IC50 = 11 nM. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50 = 56 nM. Further, GSK591 is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases[1][2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45.3 mg/mL (100 mM)


关键字: EPZ 015866 | GSK 591 | GSK591 | EPZ-015866 | Inhibitor | inhibit | GSK-3203591 | Histone Methyltransferase | GSK 3203591 | GSK-591

相关产品: BCI-121 | CPI-169 racemate | BBDDL2059 | Menin-MLL inhibitor 20 | WDR5-47 | MS023 | SNDX-5613 | CARM1-IN-3 | WDR5-0102 | XY1

相关库: Bioactive Compounds Library Max | Epigenetics Compound Library | Inhibitor Library | Target-Focused Phenotypic Screening Library | Methylation Compound Library | Reprogramming Compound Library | Stem Cell Differentiation Compound Library | NO PAINS Compound Library | Histone Modification Compound Library | Bioactive Compound Library

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