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.
More>> 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. Less<<Synonyms: 7-Hydroxy-2,3,4,5-tetrahydro-1H-[1]benzofuro[2,3-c]azepin-1-one, PKCμ Inhibitor
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Overview
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Key Specifications Table
CAS # | Empirical Formula |
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521937-07-5 | C₁₂H₁₁NO₃ |
Pricing & Availability
Catalog Number | Availability | Packaging | Qty/Pack | Price | Quantity | |
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476495-10MG |
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10 mg |
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Description | |
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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 | |
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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 | |
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CAS number | 521937-07-5 |
Form | Brown solid |
Hill Formula | C₁₂H₁₁NO₃ |
Chemical formula | C₁₂H₁₁NO₃ |
Structure formula Image | |
Quality Level | MQ100 |
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Biological Information | |
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Purity | ≥95% by HPLC |
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Packaged under inert gas | Packaged under inert gas |
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Specifications |
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Global Trade Item Number | |
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Catalog Number | GTIN |
476495-10MG | 04055977183849 |
Documentation
PKD Inhibitor, CID755673 - CAS 521937-07-5 - Calbiochem SDS
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PKD Inhibitor, CID755673 - CAS 521937-07-5 - Calbiochem Certificates of Analysis
Title | Lot Number |
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476495 |
References
Reference overview |
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LaValle, C.R., et al. 2010. BMC Chemical Biology 10, 5. Sharlow, E.R., et al. 2008. J. Biol. Chem. 283, 33516. |