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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).

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

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

207003
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
1213234-31-1C₂₀H₁₉Cl₂N₃S

Products

RéférenceConditionnement Qté
207003-10MG Flacon en verre 10 mg
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
Global Trade Item Number
Référence GTIN
207003-10MG 04055977203202

Documentation

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

Titre

Fiche de données de sécurité des matériaux (FDS) 

Calcineurin Inhibitor VIII, CN585 - CAS 1213234-31-1 - Calbiochem Certificats d'analyse

TitreNuméro de lot
207003

Références bibliographiques

Aperçu de la référence bibliographique
Erdmann, F., et al. 2010. J. Biol. Chem. 285, 1888.
Fiche technique

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 Protect from light
-20°C
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.