300817-68-9|BH3I-1|CsnPharm

CAS No.: 300817-68-9

BH3I-1 Catalog No. CSN18193

Synonyms: BHI1

BH3I-1 is an inhibitor of Bcl-xL with IC50 of 293.95 μM.

规格	价格	促销价格	库存	数量

400-920-2911

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技术信息

生物活性

描述BH3 domain-mediated dimerization plays a key role in the regulation of pro-apoptotic and anti-apoptotic activities of the Bcl-2 family proteins. BH3I-1 is a small-molecule, cell-permeable inhibitor of the BH3-domain-mediated dimerization. The K_i values of BH3I-1 for the inhibition of Bak/Bcl-xL-His6 interaction determined by FP and NMR titration assays are 2.4±0.2 and 7.8±0.9μM, respectively. The addition of BH3I-1 (50 and 200μM) dose-dependently decreased the tBid binding in vitro. Treatment of JK cells with 100μM BH3I-1 induced DNA fragmentation and an increase in caspase-3-like and caspase-9-like activities. BH3I-1 at 100µM also induced cytochrome c release in HeLa cells at 48-h post-treatment. Treatment of JK/Bcl-x_L cells with 100 µM BH3I-1 induced the appearance of sub-G1 DNA, indicative of apoptosis.^[3] BH3I-1 at a dose of 50μM promoted the apoptosis of murine bone marrow-derived eosinophils and human eosinophils isolated from the peripheral blood of healthy subjects.^[4]
作用机制BH3I-1 inhibited BH3-domain-mediated dimerization by preventing BH3 domain-mediated interaction between Bcl-2 family members.^[3]
参考文献

[1] Fullbeck M, Gebhardt N, et al. Computer-assisted identification of small-molecule Bcl-2 modulators. Comput Biol Chem. 2009 Dec;33(6):451-6.
[2] Mitsiades CS, Hayden P, et al. Bcl-2 overexpression in thyroid carcinoma cells increases sensitivity to Bcl-2 homology 3 domain inhibition. J Clin Endocrinol Metab. 2007 Dec;92(12):4845-52.
[3] Degterev A, Lugovskoy A, Cardone M, et al. Identification of small-molecule inhibitors of interaction between the BH3 domain and Bcl-xL. Nat Cell Biol. 2001;3(2):173-182. doi:10.1038/35055085
[4] Schwartz C, Willebrand R, Huber S, et al. Eosinophil-specific deletion of IκBα in mice reveals a critical role of NF-κB-induced Bcl-xL for inhibition of apoptosis. Blood. 2015;125(25):3896-3904. doi:10.1182/blood-2014-10-607788

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4981 mL
- 12.4903 mL
- 24.9806 mL
- 5 mM
- 0.4996 mL
- 2.4981 mL
- 4.9961 mL
- 10 mM
- 0.2498 mL
- 1.2490 mL
- 2.4981 mL

技术信息

CAS号

300817-68-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H14BrNO3S2

运输

蓝冰

分子量

400.31

别名

BHI1

溶解度

DMSO	62.0 mg/mL (154.9 mM) warming
Water	Insoluble
Ethanol	12.0 mg/mL (30.0 mM) warming

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