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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
BHI1
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
300817-68-9
- 规格：
5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 5 mg | 产品价格： | ￥650.0 |
|---|---|---|---|
| 规格： | 10 mg | 产品价格： | ￥1050.0 |
| 规格： | 25 mg | 产品价格： | ￥1950.0 |
| 规格： | 50 mg | 产品价格： | ￥3200.0 |
| 规格： | 100 mg | 产品价格： | ￥5200.0 |
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BH3I-1
CAS No. : 300817-68-9
MCE 国际站：BH3I-1
产品活性：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。
研究领域：Apoptosis | Metabolic Enzyme/Protease
作用靶点：Bcl-2 Family | MDM-2/p53 | E1/E2/E3 Enzyme
In Vitro: 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 Kd=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 Ki of 7.8±0.9 μM.
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