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218719

Casein Kinase I Inhibitor III, PF-4800567

Name: Casein Kinase I Inhibitor III, PF-4800567
Brand: MM

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

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About This Item

Empirical Formula (Hill Notation):

C₁₇H₁₈ClN₅O₂

CAS Number:

1188296-52-7

Molecular Weight:

359.81

UNSPSC Code:

12352200

NACRES:

NA.54

MDL number:

MFCD22123245

Assay:

≥99% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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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

InChI

1S/C17H18ClN5O2/c18-11-2-1-3-13(8-11)25-9-14-15-16(19)20-10-21-17(15)23(22-14)12-4-6-24-7-5-12/h1-3,8,10,12H,4-7,9H2,(H2,19,20,21)

InChI key

AUMDBEHGJRZSOO-UHFFFAOYSA-N

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c