218719

Casein Kinase I Inhibitor III, PF-4800567

The Casein Kinase I Inhibitor III, PF-4800567 controls the biological activity of Casein Kinase I. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : Casein Kinase I Inhibitor III, PF-4800567, 3-(3-Chlorophenoxymethyl)-1-(tetrahydropyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine, HCl, CKI Inhibitor III, PF-4800567
• Formule empirique (notation de Hill): C₁₇H₁₈ClN₅O₂
• Numéro CAS: 1188296-52-7
• Poids moléculaire : 359.81
• Numéro MDL: MFCD22123245
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.54

Propriétés

• Niveau de qualité: 100
• Pureté: ≥99% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: beige
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: wet ice
• Température de stockage: 2-8°C
• Chaîne SMILES: NC1=NC=NC2=C1C(COC3=CC=CC(Cl)=C3)=NN2C4CCOCC4

Description

Description générale

A cell-permeable pyrazolopyrimidinylamino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKIε with ~22-fold greater potency over CKIδ (IC₅₀ = 32 and 711 nM, respectively) and displays excellent selectivity among 50-kinases, with the only exception of EGFR (69% inhibition at 1 µM). Shown to preferentially block PER3 (PERIOD3) nuclear translocation in COS7-GFP-PER3-CKIε cells over CKIδ-transfected cells (IC₅₀ = 0.13 and 2.65 µM, respectively), and PER2 degradation in COS7-GFP-PER2-CKIε cells. Unlike Casein Kinase I Inhibitor II, PF-670462 (Cat. No. 218716), PF-4800567 exerts only marginal effect on circadian clock under similar conditions.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Meng, Q.J., et al. 2010. Proc. Natl. Acad. Sci. USA24, 15240.
Etchegaray, J.P., et al. 2010. PLoS One5, e10303.
Walton, K.M., et al. 2009. J. Pharmacol. Exp. Ther.330, 430.
Badura, L., et al. 2007. J. Pharmacol. Exp. Ther.322, 730.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable