500506 | EPAC Inhibitor, ESI-09

500506
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H₁₅ClN₄O2

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00506.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable propionitrile compound that targets the CBD (cAMP-binding domain) of EPAC/cAMP-GEF with 4-fold higher affinity than cAMP and selectively inhibits cAMP-dependent EPAC GEF activity (IC50 = 1.4 and 3.2 µM, respectively, against EPAC2 and EPAC1; [cAMP] = 25 µM) with much reduced potency toward cAMP-dependent PKA activity (10% and 20% inhibition at 100 µM, respectively, against 100 µM cAMP-stimulated Type Iα and IIβ PKA activity). Shown to block both basal and 8-CPT-2'-O-Me-cAMP (Cat. No. 116833) prodrug 007-AM-, but not EGF-, stimulated Akt phosphorylations in serum-starved human AsPC-1 (≥185%, ≤85%, and <10% of basal thr308/Ser473 phosphorylation, respectively, with 0, 1, 10 µM ESI-09; [007-AM] = 10 µM) and EPAC-mediated insulin secretion from rat INS-1 cells (IC50 <5 µM; [007-AM] = 10 µM).
          Catalogue Number500506
          Brand Family Calbiochem®
          SynonymsExchange Protein Directly Activated by cAMP Inhibitor, 3-(5-tert-butyl-isoxazol-3-yl)-2-((3-chlorophenyl)-hydrazono)-3-oxo-propionitrile, cAMP -GEF Inhibitor
          References
          ReferencesAlmahariq, M., et al. 2013. Mol Pharmacol. 83, 122.
          Product Information
          FormYellow powder
          Hill FormulaC₁₆H₁₅ClN₄O2
          Chemical formulaC₁₆H₁₅ClN₄O2
          Applications
          Biological Information
          Purity≥98% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Almahariq, M., et al. 2013. Mol Pharmacol. 83, 122.
          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.

          Revision28-April-2014 JSW
          SynonymsExchange Protein Directly Activated by cAMP Inhibitor, 3-(5-tert-butyl-isoxazol-3-yl)-2-((3-chlorophenyl)-hydrazono)-3-oxo-propionitrile, cAMP -GEF Inhibitor
          DescriptionA cell-permeable, propionitrile compound that targets the CBD (cAMP-binding domain) of EPAC/cAMP-GEF with 4-fold higher affinity than cAMP (IC50 = 10 vs. 39 µM, respectively, against 8-NBD-cAMP in competition EPAC2 binding assay) and selectively inhibits cAMP-dependent EPAC GEF activity (IC50 = 1.4 and 3.2 µM, respectively, against EPAC2 and EPAC1; [cAMP] = 25 µM) with much reduced potency toward cAMP-dependent PKA activity (10% and 20% inhibition at 100 µM, respectively, against 100 µM cAMP-stimulated Type Iα and IIβ PKA activity). Shown to block both basal and 8-CPT-2'-O-Me-cAMP (Cat. No. 116833) prodrug 007-AM-stimulated Akt thr308/Ser473 phosphorylations in serum-starved human pancreatic cancer AsPC-1 (%thr308/%Ser473 of basal phosphorylation = 200%/185%, 85%/65%, and <10%/<10%, respectively, with 0, 1, 10 µM ESI-09; [007-AM] = 10 µM) and rat pancreatic β-cell INS-1 without affecting EGF-stimulated Akt phosphorylations, resulting in effective inhibition of EPAC-mediated insulin secretion from INS-1 cells (by 57% and 100%, respectively, at 5 and 10 µM; [007-AM] = 10 µM) and pancreatic cancer cell invasion (~60% inhibition at 5 µM using AsPC-1 and PANC-1 cells).
          FormYellow powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₆H₁₅ClN₄O2
          Purity≥98% by HPLC
          SolubilityDMSO (100 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
          ReferencesAlmahariq, M., et al. 2013. Mol Pharmacol. 83, 122.