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

Calcineurin Inhibitor VIII, CN585, CAS 1213234-31-1, is a cell-permeable, reversible inhibitor of calcineurin-catalyzed dephosphorylation of RII phosphopeptide (Cat. No. 207008).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: PP2B Inhibitor VIII, Ca2+/Calmodulin-dependent Protein Phosphatase Inhibitor, 6-(3,4-Dichlorophenyl)-4-(N,N-dimethylaminoethylthio)-2-phenyl-pyrimidine

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207003
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Overview

Key Spec Table

CAS #Empirical Formula
1213234-31-1C₂₀H₁₉Cl₂N₃S

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207003-10MG
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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).
      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
      Global Trade Item Number
      Catalogue Number GTIN
      207003-10MG 04055977203202