中文名 | UNC3866 |
英文名 | UNC3866 |
别名 | 化合物UNC3866 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 (3S,6S,9S,12S,15S)-甲基 3-苄基-1-(4-(叔丁基)苯基)-12-(4-(二乙基氨基)丁基)-15-(羟甲基)-9-异丁基-6-甲基-1,4,7,10,13-五氧代-2,5,8,11,14-五氮杂十六烷-16-油酸 |
英文别名 | CS-2491 UNC3866 UNC 3866 UNC-3866 N-[4-(1,1-Dimethylethyl)benzoyl]-L-phenylalanyl-L-alanyl-L-leucyl-N6,N6-diethyl-L-lysyl-L-serine methyl ester L-Serine, N-[4-(1,1-dimethylethyl)benzoyl]-L-phenylalanyl-L-alanyl-L-leucyl-N6,N6-diethyl-L-lysyl-, methyl ester (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 |
CAS | 1872382-47-2 |
化学式 | C43H66N6O8 |
分子量 | 795.02 |
密度 | 1.129±0.06 g/cm3(Predicted) |
沸点 | 1034.5±65.0 °C(Predicted) |
溶解度 | DMSO: ≥ 27 mg/mL |
酸度系数 | 13.39±0.46(Predicted) |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.258 ml | 6.289 ml | 12.578 ml |
5 mM | 0.252 ml | 1.258 ml | 2.516 ml |
10 mM | 0.126 ml | 0.629 ml | 1.258 ml |
5 mM | 0.025 ml | 0.126 ml | 0.252 ml |
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