|3,6-二氯苯并噻吩-2-甲酸|CsnPharm

CAS No.: 34576-94-8

3,6-Dichlorobenzo[b]thiophene-2-carboxylic acid Catalog No. CSN27381

Synonyms: 3,6-dichloro-benzo[b]thiophene-2-Carboxylic Acid

BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Impaired branched-chain amino acids (BCAA) catabolism plays a pivotal role in the pathogenesis of metabolic and neurological diseases. The mitochondrial branched-chain α-ketoacid dehydrogenase complex (BCKDC) kinase (BDK) inhibitors that augment BCKDC flux have been shown to reduce BCAA concentrations in vivo. BT2 is a novel BDK inhibitor with an IC₅₀ value of 3.19 μM. In wild-type MEF cells, BT2 robustly stimulated BCKDC activity at concentration of 40 μM for 48 h. Administration of BT2 at 20 mg/kg/day to wild-type mice for 1 week led to nearly complete dephosphorylation and maximal activation of BCKDC in heart, muscle, kidneys, and liver with reduction in plasma BCAA concentrations^[3].
作用机制Mechanism: BT2 binds to an allosteric site in the N-terminal domain of each monomer in homodimeric BDK^[3].
参考文献

[1] Tso SC, et al. Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase. J Biol Chem. 2014 Jul 25;289(30):20583-93.
[2] Friberg A, et al. Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design. J Med Chem. 2013 Jan 10;56(1):15-30.
[3] Tso SC, Gui WJ, Wu CY, et al. Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase. J Biol Chem. 2014 Jul 25;289(30):20583-93.

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
- 4.0470 mL
- 20.2349 mL
- 40.4698 mL
- 5 mM
- 0.8094 mL
- 4.0470 mL
- 8.0940 mL
- 10 mM
- 0.4047 mL
- 2.0235 mL
- 4.0470 mL

技术信息

CAS号

34576-94-8

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

C9H4Cl2O2S

运输

蓝冰

分子量

247.10

别名

3,6-dichloro-benzo[b]thiophene-2-Carboxylic Acid

溶解度

DMSO	80.0 mg/mL (323.8 mM) warming

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

3,6-Dichlorobenzo[b]thiophene-2-carboxylic acid Catalog No. CSN27381

靶点选择性

请登录您的专属账户

确认信息