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BDK Inhibitor II, (S)-CPP，10MG，5056020001，Sigma

销售价： ¥ 1615.22 / 件

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订货号： 0BP5006

品牌型号： Sigma 5056020001

货期：询货期

最小订货量： 1件

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商品介绍
规格参数
包装参数

产品介绍 Product Description

General description

A cell-permeable chlorophenylpropionate compound that is superior to its structural analog 4PB (Cat. No. 567616) as an inhibitor against mitochondrial BCKDC (branched-chain α-ketoacid dehydrogenase complex) 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) via carboxylate oxygens-mediated hydrogen bonds, as well as hydrophobic interactions mediated by the α-chlorine and the phenyl ring, effectively blocking BDK substrate access by preventing BDK interaction with the homo-24-meric dihydrolipoyltransferase BCKDC E2 component, while exhibiting little potency against PDK2 (pyruvate dehydrogenase kinase isoform 2) or BDP (BCKD phosphatase) 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 (ED_max =160 mg/kg via i.p.; 60 min) in vivo, resulting in significant downregulation of serum BCAA (branched-chain amino acid) Leu/Ile and Val levels. Pharmacokinetic studies reveal good stability in vitro (half-life = 3.1 h and 6.8 h using murine liver S9 preparation or murine hepatocytes, respectively) and low clearance in vivo (CL/F = 0.113 mL/min; 40 mg/kg i.p.), however the compound does not penetrate tissues efficiently (V_Z/F = 20.8 mL; 40 mg/kg i.p.) and high dosages are recommended for mice treatment.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
BDK
Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Use only fresh DMSO for reconstitution.

Other Notes

Tso, S.C., et al. 2013. Proc. Natl. Acad. Sci. USA110, 9728.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

技术参数 Specifications

assay	≥98% (HPLC)
Quality Segment	100
form	oil
manufacturer/tradename	Calbiochem^®
storage condition	OK to freeze,desiccated,protect from light
color	clear colorless
solubility	DMSO: 100 mg/mL
storage temp.	−20°C
SMILES string	Cl[C@@H](Cc1ccccc1)C(=O)O
InChI	1S/C9H9ClO2/c10-8(9(11)12)6-7-4-2-1-3-5-7/h1-5,8H,6H2,(H,11,12)/t8-/m0/s1
InChI key	LIDRHDRWTSPELB-QMMMGPOBSA-N

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