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.
別名:
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
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この商品について
実験式（ヒル表記法）:
C20H19Cl2N3S
CAS番号:
分子量:
404.36
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
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
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; 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.
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)
保管分類
11 - Combustible Solids
一体何が起きているの？
WGK 2
引火点 (F)
Not applicable
引火点（°C）
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
207003-MG: + 207003-10MG:
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