Casein Kinase I Inhibitor, D4476-CAS 301836-43-1-Calbiochem

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一般描述

A cell-permeable triaryl substituted imidazolo compound that acts as a potent, reversible and relatively specific ATP-competitive inhibitor of CK1 (IC₅₀= 0.2 ?M fromS. pombe; 0.3 ?M for CK1δ) and ALK5 (IC₅₀= 0.5 ?M). A weak inhibitor of p38α MAP kinase (IC₅₀= 12 ?M) and only weakly affects the activities of a panel of kinases tested, including PKB, SGK and GSK-3β. Suppresses the site-specific phosphorylation (Ser³²²and Ser³²⁵) and nuclear exclusion of FOXO1a in H4IIE hepatoma cells. Shown to be ~10-fold more potent than IC261 (Cat. No. 400090; IC₅₀= 2.5 ?M for CK1).
A cell-permeable, reversible, potent, and relatively specific ATP-competitive inhibitor of CK1 (IC₅₀= 200 nM fromS. pombe; 0.3 ?M for CK1δ) and ALK5 (IC₅₀= 500 nM). A weak inhibitor of p38α MAP kinase (IC₅₀= 12 ?M) and several other kinases tested, including PKB, SGK, and GSK-3β. Suppresses the site-specific phosphorylation (Ser³²²and Ser³²⁵) and nuclear exclusion of FOXO1A in H4IIE hepatoma cells. Shown to be ~ 10-fold more potent than IC261 (Cat. No. 400090; IC₅₀= 2.5 ?M for CK1).

包装

1 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Target IC₅₀: 0.2 ?M against CK1 from S. pombe; 0.3 ?M for CK1δ 0.5 ?M against ALK5
Product competes with ATP.
Reversible: yes

警告

Toxicity: Standard Handling (A)

法律信息

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

基本信息

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