207003

Calcineurin Inhibitor VIII, CN585

The Calcineurin Inhibitor VIII, CN585, also referenced under CAS 1213234-31-1, controls the biological activity of Calcineurin. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinónimos: Calcineurin Inhibitor VIII, CN585, PP2B Inhibitor VIII, Ca ²⁺/Calmodulin-dependent Protein Phosphatase Inhibitor, 6-(3,4-Dichlorophenyl)-4-(N,N-dimethylaminoethylthio)-2-phenyl-pyrimidine, PP2B Inhibitor VIII, Ca²⁺/Calmodulin-dependent Protein Phosphatase Inhibitor, 6-(3,4-Dichlorophenyl)-4-(N,N-dimethylaminoethylthio)-2-phenyl-pyrimidine
• Fórmula empírica (notación de Hill): C₂₀H₁₉Cl₂N₃S
• Número de CAS: 1213234-31-1
• Peso molecular: 404.36
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: beige
• solubilidad: DMSO: 10 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: −20°C

Descripción

Descripción general

A 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; K_i = 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.

A 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; K_i = 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.

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

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

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 2
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable