化合物MS023 T6900

Product Introduction
Bioactivity


英文名: MS023

描述: MS023 是一种有效的、选择性的、细胞活性的 I 型 PRMT 抑制剂，对 PRMT1、PRMT3、PRMT4、PRMT6和 PRMT8的 IC50分别为 30、119、83、4 和 5 nM。

激酶实验: PRMT Biochemical Assays: A scintillation proximity assay (SPA) is used for assessing the effect of test compounds on inhibiting the methyl transfer reaction catalyzed by PRMTs. In brief, the tritiated S-adenosyl-L-methionine (3H-SAM) is used as the donor of methyl group. The (3H) methylated biotin labeled peptide is captured in a streptavidin/scintillant-coated microplate, which brings the incorporated 3H-methyl and the scintillant to close proximity resulting in light emission that is quantified by tracing the radioactivity signal (counts per minute) as measured by a TopCount NXT Microplate Scintillation and Luminescence Counter. When necessary, nontritiated SAM is used to supplement the reactions. The IC50 values are determined under balanced conditions at Km concentrations of both substrate and cofactor by titration of test compounds in the reaction mixture.

体外活性: MS023 potently reduces cellular levels of H4R3me2a in MCF7 and HEK293 cells by inhibiting PRMT1/6 methyltransferase activity with IC50 of 9 nM and 56 nM, respectively. MS023 also inhibits cell growth and potentially induces growth arrest and flattening morphology at low concentrations. [1]

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

溶解度: Ethanol : 53 mg/mL (184.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 53 mg/mL (184.4 mM)


关键字: Inhibitor | MS 023 | MS023 | MS-023 | inhibit | Histone Methyltransferase

相关产品: MRTX-1719 | (Iso)-MS4322 | DW14800 | SETDB1-TTD-IN-1 | MS0124 | TC-E 5003 | M‑89 | CARM1 degrader-1 | SETD7-IN-1 | GSK3368715 dihydrochloride

相关库: Anti-Aging Compound Library | Inhibitor Library | Epigenetics Compound Library | Target-Focused Phenotypic Screening Library | Stem Cell Differentiation Compound Library | Reprogramming Compound Library | Methylation Compound Library | Histone Modification Compound Library | Chromatin Modification Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途