数量	产品目录编号	订购说明	数量 / 包装	公开价
			96-Well Plate

数量	产品目录编号	订购说明	数量 / 包装	公开价
	48-602MAG	Buffer Detection Kit for Magnetic Beads	1 Kit

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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
参考
Data Sheet

同义词: BCKD Kinase Inhibitor II, Branched-Chain α-Ketoacid Dehydrogenase Kinase Inhibitor II, (S)-α-Chloro-phenylpropionic acid

Primary Target: BDK

View Products on Sigmaaldrich.com

Recommended Products

概述

Replacement Information

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	正在查询供货情况...... — 目前缺货有货停产少量现货供货情况有待确认登录查看库存有货目前缺货有货其余：另行通知其余：另行通知另行通知联系客户服务 Contact Customer Service 联系客户服务联系客户服务	玻璃瓶	10 mg	正在检索价格...... 无法检索价格。最小订购数量为倍数 Maximum Quantity is 以订单确认为准更多信息您节约了 ()。 — Request Pricing 登录查看价格	查看库存情况 —	添加到收藏夹添加到收藏夹添加到我的收藏夹

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 (ED_max =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

Applications

Biological Information
Primary Target	BDK
Purity	≥98% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	-20°C
Protect from Light	Protect from light
Protect from Moisture	Protect from moisture
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
5.05602.0001	04055977243406

Documentation

BDK Inhibitor II, (S)-CPP - CAS 41998-38-3 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

参考

参考信息概述
Tso, S.C., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 9728.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	07-March-2014 JSW
Synonyms	BCKD Kinase Inhibitor II, Branched-Chain α-Ketoacid Dehydrogenase Kinase Inhibitor II, (S)-α-Chloro-phenylpropionic acid
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.
Form	Clear, colorless oil
Intert gas (Yes/No)	Packaged under inert gas
CAS number	41998-38-3
Chemical formula	C₉H₉ClO₂
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
Storage	Protect from moisture Protect from light -20°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Toxicity	Standard Handling
References	Tso, S.C., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 9728.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Other Kinase Inhibitors

此产品已添加到您的购物车。