A366 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。

Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. Decreases levels of lysine 9 dimethylation on histone H3 (H3K9Me2) in PC3 cells.

A-366对异种移植白血病模型中肿瘤的生长产生抑制作用.

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。

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

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)

1527503-11-2

C19H27N3O2

329.444

A366;A 366

DMSO:32.9 mg/mL (100 mM)
1eq. HCl:32.9 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years