300817-68-9
300817-68-9 结构式
基本信息
BHI1
BH 3I1
BH3I 1
BH3I1
5-(p-Bromobenzylidine)-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid
5-(p-Bromobenzylidene)-a-isopropyl-4-oxo-2-thioxo-3-thiazolidine acetic acid
3-Thiazolidineacetic acid, 5-[(4-bromophenyl)methylene]-α-(1-methylethyl)-4-oxo-2-thioxo-
物理化学性质
常见问题列表
|
Bcl-2
|
Bcl-xL
|
Bim
|
Bak
|
p53/mDM2 5.3 μM (Kd) |
BH3I-1, while inhibiting its reported target Bcl-2/Bim and Bcl-xL/Bim, shows significant inhibition of both the p53/hDM2 and p300/Hif-1α interactions. This surprising promiscuity, displays by a well studied compound leads to further interrogate the p53/hDM2 interaction utilizing a standard fluorescence polarization (FP) assay with purified protein. The results from the FP assay validates the split-luciferase screen and demonstrates that BH3I-1 has a K d =5.3 μM against the p53/mDM2 pair, which is comparable to its low micromolar potency reported for the BH3 family of receptors. BH3I-1 inhibits interaction between the BH3 domain and Bcl-xL. NMR analyses reveal that BH3I-1 targets the BH3-binding pocket of Bcl-xL with a K i of 7.8±0.9 μM.