505602 Sigma-AldrichBDK Inhibitor II, (S)-CPP - CAS 41998-38-3 - Calbiochem
A cell-permeable inhibitor of mitochondrial branched-chain α-ketoacid dehydrogenase complex (BCKDC) regulatory kinase BDK (IC₅₀ = 6.3 µM).
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同义词: BCKD Kinase Inhibitor II, Branched-Chain α-Ketoacid Dehydrogenase Kinase Inhibitor II, (S)-α-Chloro-phenylpropionic acid
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概述
重要规格表
| CAS # | Empirical Formula |
|---|---|
| 41998-38-3 | C₉H₉ClO₂ |
价格及供货情况
| 产品目录编号 | 库存情况 | 包装 | 数量 / 包装 | 价格 | 数量 | |
|---|---|---|---|---|---|---|
| 5.05602.0001 |
|
玻璃瓶 | 10 mg |
|
— |
| Description | |
|---|---|
| Overview | A cell-permeable chlorophenylpropionate compound that is superior to its structural analog 4PB (Cat. No. 567616) as an inhibitor against mitochondrial branched-chain α-ketoacid dehydrogenase complex (BCKDC) regulatory kinase BDK (BCKD kinase; IC50 = 6.3 vs. 53.1 µM) due to much optimized affinity toward the BDK N-terminal allosteric site (Kd = 2.4 vs. 5.7 µM), effectively blocking BDK substrate access by preventing BDK interaction with the homo-24-meric dihydrolipoyltransferase BCKDC E2 component, while exhibiting little potency against PDK2 or BCKD phosphatase BDP even at concentrations as high as 1 mM (<10% inhibition). Shown to effectively reduce E1-α Ser293 phosphorylation with concomitant BCKDC activity upregulation in multiple tissues in mice (EDmax =160 mg/kg via i.p.) in vivo. Despite good stability and low in vivo clearance , high doses are recommended for mice treatment due to low tissue penetration efficiency. |
| Catalogue Number | 505602 |
| Brand Family | Calbiochem® |
| Synonyms | BCKD Kinase Inhibitor II, Branched-Chain α-Ketoacid Dehydrogenase Kinase Inhibitor II, (S)-α-Chloro-phenylpropionic acid |
| References | |
|---|---|
| References | Tso, S.C., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 9728. |
| Product Information | |
|---|---|
| CAS number | 41998-38-3 |
| Form | Clear, colorless oil |
| Hill Formula | C₉H₉ClO₂ |
| Chemical formula | C₉H₉ClO₂ |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Primary Target | BDK |
| Purity | ≥98% by HPLC |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| 产品目录编号 | GTIN |
| 5.05602.0001 | 04055977243406 |