中文同义词:
UNC3866游离态;N-[4-(1,1-二甲基乙基)苯甲酰基]-L-苯丙氨酰基-L-丙氨酰基-L-亮氨酰-N6,N6-二乙基-L-赖氨酰-L-丝氨酸甲酯;化合物UNC3866
英文同义词:
UNC3866;N-[4-(1,1-Dimethylethyl)benzoyl]-L-phenylalanyl-L-alanyl-L-leucyl-N6,N6-diethyl-L-lysyl-L-serine methyl ester;CS-2491;UNC 3866;UNC-3866;(3S,6S,9S,12S,15S)-Methyl 3-benzyl-1-(4-(tert-butyl)phenyl)-12-(4-(diethylamino)butyl)-15-(hydroxymethyl)-9-isobutyl-6-methyl-1,4,7,10,13-pentaoxo-2,5,8,11,14-pentaazahexadecan-16-oate;L-Serine, N-[4-(1,1-dimethylethyl)benzoyl]-L-phenylalanyl-L-alanyl-L-leucyl-N6,N6-diethyl-L-lysyl-, methyl ester
沸点
1034.5±65.0 °C(Predicted)
密度
1.129±0.06 g/cm3(Predicted)
储存条件
Sealed in dry,Store in freezer, under -20°C
酸度系数(pKa)
13.39±0.46(Predicted)
生物活性
UNC3866 是一种有效的 CBX7-H3 拮抗剂，IC50 为 66±1.2 nM。
体外研究
UNC3866, a potent antagonist of the methyl-lysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently with a K d of 100 nM for each, and is 6- to 18-fold selective versus seven other CBX and CDY chromodomains while being highly selective versus >250 other protein targets. UNC3866 inhibits PC3 cell proliferation, a known CBX7 phenotype, while UNC4219, a methylated negative control compound, has negligible effects. UNC3866 is a potent and cellularly active antagonist of PRC1 chromodomains. UNC3866 is the most potent ligand reported for CBX7 with a K d of 97±2.4 nM. UNC3866 is equipotent for CBX4, which is most similar to CBX7, while it is 18-, 6- and 12-fold selective for CBX4/7 over CBX2, -6 and -8, respectively. Additionally, UNC3866 is 65-fold selective for CBX4/7 over CDY1 and 9-fold selective for CBX4/7 over CDYL1b and CDYL2.
