化合物A366 T3624

Product Introduction
Bioactivity


英文名: A-366

描述: A-366 是一种高选择性的肽竞争性组蛋白甲基转移酶 G9a 抑制剂，对 G9a 和 GLP 的 IC50分别为 3.3 和 38 nM。它比其他 21 种甲基转移酶具有 1000 倍以上的选择性。它是 Spindlin1-H3K4me3相互作用的抑制剂，IC50为182.6 nM。它对人 H3R 表现出很高的亲和力，Ki 值为 17 nM，在组胺能和多巴胺能受体家族的亚群间表现出亚型选择性。

细胞实验: PC-3 prostate adenocarcinoma cells are incubated in triplicate with DMSO or the indicated concentrations of A-366 or UNC0638 for 72 hours. H3K9me2 levels are assessed by In-Cell Western assay. (Only for Reference)

激酶实验: 7.5× compounds are added to a 96-well PolyPlate containing 60 μL of Buffer per well with substrates CoA (200 μM), ATP (400 μM), and [14C]citrate. Reaction is started with 4 μL (300 ng/well) ACL, and the plate is incubated at 37°C for 3 h. Th

体外活性: A-366对异种移植白血病模型中肿瘤的生长产生抑制作用.

体内活性: 对肿瘤细胞生长而言,A-366比其他一些G9a/GLP小分子化合物抑制剂具有更少的毒性效应,而对H3K9me2的甲基化效果无差别,在体外用A-366处理各种白血病细胞株,这些肿瘤细胞将产生显著的分化和形态上的变化。

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

溶解度: 1eq. HCl : 32.9 mg/mL (100 mM)
DMSO : 32.9 mg/mL (100 mM)


关键字: epigenetics | interaction | H3K4me3 | A-366 | inhibit | Epigenetic Reader Domain | selective | peptide-competitive | Inhibitor | methyltransferase | cells

相关产品: PNZ5 | PROTAC BRD9 Degrader-6 | Cycloastragenol | I-CBP112 | Curcumin | GNE-375 | ACBI1 | BY27 | FL-411 | UNC926

相关库: Anti-Aging Compound Library | Glycometabolism Compound Library | Inhibitor Library | Highly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library | Reprogramming Compound Library | Methylation Compound Library | Stem Cell Differentiation Compound Library | NO PAINS 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