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

207003
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Empirical FormulaCAS #
C₂₀H₁₉Cl₂N₃S1213234-31-1

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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
      Quality LevelMQ100
      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

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

      Title

      Safety Data Sheet (SDS) 

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