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476495 PKD Inhibitor, CID755673 - CAS 521937-07-5 - Calbiochem

476495
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
521937-07-5C₁₂H₁₁NO₃

Products

Catalogue NumberPackaging Qty/Pack
476495-10MG 10 mg
Description
OverviewA 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 Number476495
Brand Family Calbiochem®
Synonyms7-Hydroxy-2,3,4,5-tetrahydro-1H-[1]benzofuro[2,3-c]azepin-1-one, PKCμ Inhibitor
References
ReferencesLaValle, C.R., et al. 2010. BMC Chemical Biology 10, 5.
Sharlow, E.R., et al. 2008. J. Biol. Chem. 283, 33516.
Product Information
CAS number521937-07-5
FormBrown solid
Hill FormulaC₁₂H₁₁NO₃
Chemical formulaC₁₂H₁₁NO₃
Structure formula ImageStructure formula Image
Quality LevelMQ100
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 InstructionsFollowing 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

Documentation

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

Title

Safety Data Sheet (SDS) 

PKD Inhibitor, CID755673 - CAS 521937-07-5 - Calbiochem Certificates of Analysis

TitleLot Number
476495

References

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

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.

Revision15-September-2010 RFH
Synonyms7-Hydroxy-2,3,4,5-tetrahydro-1H-[1]benzofuro[2,3-c]azepin-1-one, PKCμ Inhibitor
DescriptionA 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).
FormBrown solid
Intert gas (Yes/No) Packaged under inert gas
CAS number521937-07-5
Chemical formulaC₁₂H₁₁NO₃
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesLaValle, C.R., et al. 2010. BMC Chemical Biology 10, 5.
Sharlow, E.R., et al. 2008. J. Biol. Chem. 283, 33516.