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.

• 別名: 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
• 実験式（ヒル表記法）: C₁₇H₁₈ClN₅O₂
• CAS番号: 1188296-52-7
• 分子量: 359.81
• MDL番号: MFCD22123245
• UNSPSCコード: 12352200
• NACRES: NA.54

特性

• 品質水準: 100
• アッセイ: ≥99% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: beige
• 溶解性: DMSO: 50 mg/mL
• 輸送温度: wet ice
• 保管温度: 2-8°C
• SMILES記法: 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)

詳細

詳細

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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable