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PKD Inhibitor, CID755673-CAS 521937-07-5-Calbiochem

品牌
Sigma-Aldrich
CAS
521937-07-5
货号
476495
规格纯度
The PKD Inhibitor, CID755673, also referenced under CAS 521937-07-5, controls the biological activity of PKD. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
参考价格
3543.57 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

A cell-permeable benzoxoloazepinolone compound that effectively inhibits syntide-2 (Cat. No. 05-23-4910) phosphorylation by all three PKD/PKCµ isoforms 1, 2, & 3 (IC50 = 182, 280, and 227 nM, respectively), while exhibiting ≥30-fold less potency towards Cdk activating kinase, Plk1, CaMKIIα, as well as 44 other kinases, 33 of which are not significantly inhibited even at concentrations as high as 10 µM, including Akt1/2 and PKCα/β/δ/ζ. Shown to block PMA- (Cat. No. 524400) induced PKD1 phosphorylation on Ser742 and Ser916 in LNCaP cells, PMA-induced HCAS5 nuclear export in HeLa cells, as well as other PKD-mediated cellular responses. The mode of inhibition is demonstrated not to be ATP-competitive in nature. Also reported to inhibit MAPKAPK2, GSK-3β, CKIδ, MK5 (PRAK), CDK2, and Erk1 kinase activity at much elevated concentrations (% inhibition by 10 µM inhibitor = 95, 86, 82, 75, 71, and 50, respectively).
A cell-permeable benzoxoloazepinolone compound that effectively inhibits syntide-2 (Cat. No. 05-23-4910) phosphorylation by all three PKD/PKCµ isoforms 1, 2, & 3 (IC50 = 182, 280, and 227 nM, respectively), while exhibiting ≥30-fold less potency towards Cdk activating kinase, Plk1, CaMKIIα, as well as 44 other kinases, 33 of which are not significantly inhibited even at concentrations as high as 10 µM, including Akt1/2 and PKCα/β/δ/ζ. Shown to block PMA- (Cat. No. 524400) induced PKD1 phosphorylation on Ser742 and Ser916 in LNCaP cells, PMA-induced HCAS5 nuclear export in HeLa cells, as well as other PKD-mediated cellular responses. The mode of inhibition is demonstrated not to be ATP-competitive in nature. Also reported to inhibit MAPKAPK2, GSK-3β, CKIδ, MK5 (PRAK), CDK2, and Erk1 kinase activity at much elevated concentrations (% inhibition by 10 µM inhibitor = 95, 86, 82, 75, 71, and 50, respectively).

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

LaValle, C.R., et al. 2010. BMC Chemical Biology10, 5.
Sharlow, E.R., et al. 2008. J. Biol. Chem.283, 33516.

法律信息

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

基本信息

经验(实验)分子式C12H11NO3
分子量217.22
MDL编号MFCD03828155

产品性质

质量水平100
测定≥95% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 brown
溶解性DMSO: 50 mg/mL
运输ambient
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3

Sigma-Aldrich

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