BH3I-1
|
|
|
- CAS号:
- 300817-68-9
- 英文名:
- BH3I-1
- 英文别名:
- BHI1;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;2-(5-(4-Bromobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)-3-methylbutanoic acid;3-Thiazolidineacetic acid, 5-[(4-bromophenyl)methylene]-α-(1-methylethyl)-4-oxo-2-thioxo-;MDM-2/p53,BH3I 1,Inhibitor,Ubiquitin ligase,BH3I-1,E3 ligating enzyme,Ubiquitin conjugating enzyme,BH3I1,E2 conjugating enzyme,Bcl-2 Family,BHI 1,E1 activating enzyme,inhibit,BHI-1,BH 3I1,E1/E2/E3 Enzyme,Ubiquitin activating enzyme,BH-3I-1
- 中文名:
- BH3I-1
- 中文别名:
- 化合物BH3I1;BH3I-1游离态;2-(5-(4-溴苯基亚甲基)-4-氧代-2-硫代噻唑-3-基)-3-甲基丁酸
- CBNumber:
- CB6497943
- 分子式:
- C15H14BrNO3S2
- 分子量:
- 400.31
- MOL File:
- 300817-68-9.mol
|
|
|
BH3I-1化学性质
-
沸点:
-
535.2±60.0 °C(Predicted)
-
|
-
密度:
-
1?+-.0.1 g/cm3(Predicted)
-
|
-
储存条件:
-
Sealed in dry,2-8°C
-
|
-
溶解度:
-
DMSO: >10 mg/mL, soluble
-
|
-
形态:
-
powder, yellow
-
|
-
酸度系数(pKa):
-
3.39±0.10(Predicted)
-
|
BH3I-1性质、用途与生产工艺
BH3I-1 是一种 Bcl-2家族 拮抗剂，抑制 Bak BH3 肽与 Bcl-xL 结合，Ki 为 2.4±0.2 μM。BH3I-1 作用于 p53/mDM2，Kd 为 5.3 μM。
|
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.
BH3I-1
上下游产品信息
上游原料
下游产品
300817-68-9, BH3I-1 相关搜索:
- API
- 药靶配体
- 抑制剂
- 标准品
- C15H14BrNS2O3
- 2-(5-(4-溴苯基亚甲基)-4-氧代-2-硫代噻唑-3-基)-3-甲基丁酸
- 化合物BH3I1
- BH3I-1游离态
- 300817-68-9
- MDM-2/p53,BH3I 1,Inhibitor,Ubiquitin ligase,BH3I-1,E3 ligating enzyme,Ubiquitin conjugating enzyme,BH3I1,E2 conjugating enzyme,Bcl-2 Family,BHI 1,E1 activating enzyme,inhibit,BHI-1,BH 3I1,E1/E2/E3 Enzyme,Ubiquitin activating enzyme,BH-3I-1
- 2-(5-(4-Bromobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)-3-methylbutanoic 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-
- BHI1;BH 3I1
- BHI1
- BH3I 1 ;BH3I1
- 5-(p-Bromobenzylidine)-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid