Application
一种有效的选择性的HMTase(组蛋白赖氨酸甲基转移酶)抑制剂，作用于G9a和GLP，IC50分别为<15nM和19nM。
UNC0638 is an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 treatment of a variety of cell lines resulted in lower global H3K9me2 levels, equivalent to levels observed for small hairpin RNA knockdown of G9a and GLP with the functional potency of UNC0638 being well separated from its toxicity. UNC0638 markedly reduced the clonogenicity of MCF7 cells, reduced the abundance of H3K9me2 marks at promoters of known G9a-regulated endogenous genes and disproportionately affected several genomic loci encoding microRNAs.
UNC0638是G9a和GLP的抑制剂，在广泛的表观遗传和非表观遗传靶标上均具有出色的效能和选择性。 UNC0638处理多种细胞系可导致较低的整体H3K9me2水平，相当于在G9a和GLP的小发夹RNA敲低中观察到的水平，而UNC0638的功能效价与其毒性完全分开。 UNC0638显着降低了MCF7细胞的克隆形成能力，降低了已知G9a调节的内源基因启动子上H3K9me2标记的丰度，并且不成比例地影响了几个编码microRNA的基因组位点。
Properties
| Iupac Name： | 2-cyclohexyl-N-(1-isopropyl-4-piperidinyl)-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine |
| Inchi Code | 1S/C30H47N5O2/c1-22(2)35-17-12-24(13-18-35)31-30-25-20-27(36-3)28(37-19-9-16-34-14-7-8-15-34)21-26(25)32-29(33-30)23-10-5-4-6-11-23/h20-24H,4-19H2,1-3H3,(H,31,32,33) |
| Inchi Key | QOECJCJVIMVJGX-UHFFFAOYSA-N |
安全信息
危险分类
Acute Tox. 2 Oral - Aquatic Chronic 4
储存分类代码
6.1A - Combustible, acute toxic Cat. 1 and 2 / very toxic hazardous materials
