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476495 Sigma-AldrichPKD Inhibitor, CID755673 - CAS 521937-07-5 - Calbiochem

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.

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

MSDS
分析证书
参考
Data Sheet

同义词: 7-Hydroxy-2,3,4,5-tetrahydro-1H-[1]benzofuro[2,3-c]azepin-1-one, PKCμ Inhibitor

Recommended Products

概述

Replacement Information

重要规格表

CAS #	Empirical Formula
521937-07-5	C₁₂H₁₁NO₃

价格及供货情况

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Description
Overview	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).
Catalogue Number	476495
Brand Family	Calbiochem®
Synonyms	7-Hydroxy-2,3,4,5-tetrahydro-1H-[1]benzofuro[2,3-c]azepin-1-one, PKCμ Inhibitor

References
References	LaValle, C.R., et al. 2010. BMC Chemical Biology 10, 5. Sharlow, E.R., et al. 2008. J. Biol. Chem. 283, 33516.

Product Information
CAS number	521937-07-5
Form	Brown solid
Hill Formula	C₁₂H₁₁NO₃
Chemical formula	C₁₂H₁₁NO₃
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Purity	≥95% by HPLC

Physicochemical Information

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	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months 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
476495-10MGCN	04055977183849

Documentation

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

职位
物料安全数据表 (MSDS)

PKD Inhibitor, CID755673 - CAS 521937-07-5 - Calbiochem 分析证书

标题	批号
476495	输入批号

参考

参考信息概述
LaValle, C.R., et al. 2010. BMC Chemical Biology 10, 5. Sharlow, E.R., et al. 2008. J. Biol. Chem. 283, 33516.

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	15-September-2010 RFH
Synonyms	7-Hydroxy-2,3,4,5-tetrahydro-1H-[1]benzofuro[2,3-c]azepin-1-one, PKCμ Inhibitor
Description	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).
Form	Brown solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	521937-07-5
Chemical formula	C₁₂H₁₁NO₃
Structure formula
Purity	≥95% by HPLC
Solubility	DMSO (50 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Standard Handling
References	LaValle, C.R., et al. 2010. BMC Chemical Biology 10, 5. Sharlow, E.R., et al. 2008. J. Biol. Chem. 283, 33516.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Calmodulin-Dependent Protein Kinase (CaM Kinase) Inhibitors

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