207003 Calcineurin Inhibitor VIII, CN585 - CAS 1213234-31-1 - Calbiochem

207003
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₀H₁₉Cl₂N₃S 1213234-31-1

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      207003-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable pyrimidine compound that is shown to inhibit the calcineurin (PP2B)-catalyzed dephosphorylation of RII phosphopeptide (Cat. No. 207008), but not pNPP (Cat. Nos. 4876, 487600, 487655, 487663, 487666), in a reversible, calmodulin-independent, and substrate-noncompetitive manner (IC50 = 3.5 µM; Ki = 3.8 µM), while exhibiting little activity against PP1, PP2A, or PP2C even at concentrations as high as 100 µM. Unlike CsA (Cat. No. 239835) and FK506 (Cat. No. 342500), CN585 does not require Cyp A (Cat. No. 239777) and FKBP family immunophilins for PP2B inhibition, nor does CN585 inhibit the peptidyl prolyl cis/trans isomerase (PPIase) activity of Cyp18, FKBP12 (Cat. No. 325902), and Pin1, although binding studies indicate that CN585 and Cyp18/CsA target a common or overlapping binding sites on the catalytic subunit of PP2B. CN585, at 30 µM, is shown to effectively block NFAT nuclear translocation in HeLa cells, NFAT transcription activity in Jurkat cells (IC50 = 10 µM), as well as IL-2 production in PBMC (IC50 = 13 µM) upon PMA/ionomycin stimulation.
          Catalogue Number207003
          Brand Family Calbiochem®
          SynonymsPP2B Inhibitor VIII, Ca2+/Calmodulin-dependent Protein Phosphatase Inhibitor, 6-(3,4-Dichlorophenyl)-4-(N,N-dimethylaminoethylthio)-2-phenyl-pyrimidine
          References
          ReferencesErdmann, F., et al. 2010. J. Biol. Chem. 285, 1888.
          Product Information
          CAS number1213234-31-1
          FormBeige solid
          Hill FormulaC₂₀H₁₉Cl₂N₃S
          Chemical formulaC₂₀H₁₉Cl₂N₃S
          Structure formula ImageStructure formula Image
          Applications
          ApplicationCalcineurin Inhibitor VIII, CN585, CAS 1213234-31-1, is a cell-permeable, reversible inhibitor of calcineurin-catalyzed dephosphorylation of RII phosphopeptide (Cat. No. 207008).
          Biological Information
          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 -20°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) 

          Certificates of Analysis

          TitleLot Number
          207003

          References

          Reference overview
          Erdmann, F., et al. 2010. J. Biol. Chem. 285, 1888.
          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.

          Revision05-April-2011 RFH
          SynonymsPP2B Inhibitor VIII, Ca2+/Calmodulin-dependent Protein Phosphatase Inhibitor, 6-(3,4-Dichlorophenyl)-4-(N,N-dimethylaminoethylthio)-2-phenyl-pyrimidine
          DescriptionA cell-permeable pyrimidine compound that is shown to inhibit the calcineurin (PP2B)-catalyzed dephosphorylation of RII phosphopeptide (Cat. No. 207008), but not pNPP (Cat. Nos. 4876, 487600, 487655, 487663, 487666), in a reversible, calmodulin-independent, and substrate-noncompetitive manner (IC50 = 3.5 µM; Ki = 3.8 µM), while exhibiting little activity against PP1, PP2A, or PP2C even at concentrations as high as 100 µM. Unlike CsA (Cat. No. 239835) and FK506 (Cat. No. 342500), CN585 does not require Cyp A (Cat. No. 239777) and FKBP family immunophilins for PP2B inhibition, nor does CN585 inhibit the peptidyl prolyl cis/trans isomerase (PPIase) activity of Cyp18, FKBP12 (Cat. No. 325902), and Pin1, although binding studies indicate that CN585 and Cyp18/CsA target a common or overlapping binding sites on the catalytic subunit of PP2B. CN585, at 30 µM, is shown to effectively block NFAT nuclear translocation in HeLa cells, NFAT transcription activity in Jurkat cells (IC50 = 10 µM), as well as IL-2 production in PBMC (IC50 = 13 µM) upon PMA/ionomycin stimulation.
          FormBeige solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1213234-31-1
          Chemical formulaC₂₀H₁₉Cl₂N₃S
          Structure formulaStructure formula
          SolubilityDMSO (10 mg/ml)
          Storage -20°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
          ReferencesErdmann, F., et al. 2010. J. Biol. Chem. 285, 1888.