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

476495
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Empirical FormulaCAS #
C₁₂H₁₁NO₃ 521937-07-5

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476495-10MG
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      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.