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.

• Synonym(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
• Empirical Formula (Hill Notation): C₁₇H₁₈ClN₅O₂
• CAS Number: 1188296-52-7
• Molecular Weight: 359.81
• MDL number: MFCD22123245
• UNSPSC Code: 12352200
• NACRES: NA.54

Properties

• Quality Level: 100
• Assay: ≥99% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: beige
• solubility: DMSO: 50 mg/mL
• shipped in: wet ice
• storage temp.: 2-8°C
• SMILES string: NC1=NC=NC2=C1C(COC3=CC=CC(Cl)=C3)=NN2C4CCOCC4

Description

General description

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable