| 产品介绍 |
UNC1215是选择性MBT (恶性脑瘤)拮抗剂，与L3MBTL3结合，IC50为40 nM，Kd为120 nM。 |
| 生化机理 |
UNC1215 binds L3MBTL3 with a K(d) of 120 nM, competitively displacing mono- or dimethyllysine-containing peptides, and is greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family while also demonstrating selectivity against more than 200 other reader domains examined. X-ray crystallography identified a unique 2:2 polyvalent mode of interaction between UNC1215 and L3MBTL3. In cells, UNC1215 is nontoxic and directly binds L3MBTL3 via the Kme-binding pocket of the MBT domains. UNC1215 increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutants that disrupt the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization. |
| 别名 |
UNC 1215;UNC-1215; 1,1'-[2-(苯基氨基)-1,4-亚苯基]二[1-[4-(1-吡咯烷基)-1-哌啶基]甲酮];UNC 1215;UNC-1215; 1,1'-[2-(Phenylamino)-1,4-phenylene]bis[1-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone]; 2-Phenylamino-1,4-[4-(pyrrolidinyl)piperidinyl)benzamide |
