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BT2
CAS No. 34576-94-8
BT2 ( —— )
产品货号. M22491 CAS No. 34576-94-8
BT2 是一种 BCKDC 激酶 (BDK) 抑制剂，IC50 为 3.19 μM。 BT2（化合物 4）也是一种有效的选择性 Mcl-1 抑制剂，Ki 值为 59 μM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 10MG | ￥316 | 有现货 |
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| 25MG | ￥470 | 有现货 |
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| 50MG | ￥583 | 有现货 |
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| 100MG | ￥851 | 有现货 |
|
| 500MG | ￥2074 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称BT2
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述BT2 是一种 BCKDC 激酶 (BDK) 抑制剂，IC50 为 3.19 μM。 BT2（化合物 4）也是一种有效的选择性 Mcl-1 抑制剂，Ki 值为 59 μM。
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产品描述BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 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 treatment reduces the protein levels of BDK in kidneys and heart[1]. The -fold activation of BCKDC activity in the above tissues correlates with decreased phosphorylation in heart, muscle, and kidney after the long term BT2 treatment. BT2 (20 mg/kg/day; intraperitoneal injection; daily; for 7 days; C57BL/6J male mice) treatment robustly enhances BCKDC activity in the heart (12.3-fold) compared with the vehicle-treated animals. Less activation is obtained in muscle and kidney at 3.6- and 3.8-fold, respectively.
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体外实验——
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体内实验BT2 (20 mg/kg/day; intraperitoneal injection; daily; for 7 days; C57BL/6J male mice) treatment robustly enhances BCKDC activity in the heart (12.3-fold) compared with the vehicle-treated animals. Less activation is obtained in muscle and kidney at 3.6- and 3.8-fold, respectively. The -fold activation of BCKDC activity in the above tissues correlates with decreased phosphorylation in heart, muscle, and kidney after the long term BT2 treatment. BT2 treatment reduces the protein levels of BDK in kidneys and heart. Animal Model:C57BL/6J male mice (8-10-week-old) Dosage:20 mg/kg/day Administration:Intraperitoneal injection; daily; for 1 week Result:BCKDC activity was robustly (12.3-fold) enhanced in the heart compared with the vehicle-treated animals. Less activation was obtained in muscle and kidney at 3.6- and 3.8-fold, respectively. The protein levels of BDK in kidneys and heart were reduced to averages of 39 and 24%, respectively.
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同义词——
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通路Angiogenesis
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靶点Bcl-2
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受体BDK|Mcl-1
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研究领域——
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适应症——
化学信息
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CAS Number34576-94-8
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分子量247.1
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分子式C9H4Cl2O2S
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纯度>98% (HPLC)
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溶解度DMSO:83.33 mg/mL (337.23 mM; Need ultrasonic)
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SMILESOC(=O)c1sc2cc(Cl)ccc2c1Cl
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
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.
产品手册
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