UNC0638  1255580-76-7

 UNC-0638
分子式：C30H47N5O2   分子量：509.73
 
產品描述
UNC0638 是選擇性組蛋白賴氨酸甲基轉移酶（HMTase）抑制劑，作用于G9a和GLP，IC50分別為< 15 nM 和 19 nM，有效且選擇性地作用于多種表觀遺傳和非表觀遺傳靶點。
靶點
G9a
GLP
       
IC50
< 15 nM
19 nM
       
體外研究
UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP, with a toxicity/function ratio of >100, compared to <6 for BIX01294. UNC0638 is a selectivite inhibitor of G9a and GLP over a wide range of epigenetic and non-epigenetic targets. UNC0638 is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. In MDA-MB-231 cells, UNC0638 (48 h exposure) reduces H3K9me2 levels in a concentration-dependent manner with an IC50 of 81 nM. UNC0638 treatment of a variety of cell lines results 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 reduces the clonogenicity of MCF7 cells, reduces the abundance of H3K9me2 marks at promoters of known G9a-regulated endogenous genes and disproportionay affected several genomic loci encoding microRNAs. In mouse embryonic stem cells, UNC0638 reactivates G9a-silenced genes and a retroviral reporter gene in a concentration-dependent manner without promoting differentiation.
體內研究
 
溶解性
DMSO 100 mM，乙醇 100 mM
穩定性
2年 -20°C粉狀，6月-80°C溶于DMSO