207003

Inhibitor kalcyneuryny 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.

• Synonim(y): Inhibitor PP2B VIII, inhibitor fosfatazy białkowej ^{zależnej od} Ca ^{2+/kalmoduliny}, 6-(3,4-dichlorofenylo)-4-(N,N-dimetyloaminoetylotio)-2-fenylo-pirymidyna, Inhibitor PP2B VIII, inhibitor fosfatazy białkowej zależnej od ^{Ca2+/kalmoduliny}, 6-(3,4-dichlorofenylo)-4-(N,N-dimetyloaminoetylotio)-2-fenylo-pirymidyna
• Wzór empiryczny (zapis Hilla): C₂₀H₁₉Cl₂N₃S
• Numer CAS: 1213234-31-1
• Masa cząsteczkowa: 404.36
• MDL number: MFCD23102145
• NACRES: NA.77
• UNSPSC Code: 12352200
• Form: solid
• Storage condition: OK to freeze, protect from light

Właściwości

• Quality Segment: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: beige
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Opis

General description

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.

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable