Casein Kinase I Inhibitor VIII

A cell-permeable pyridyl-pyrrolopyridinone compound that acts as an ATP site-targeting, γ isotype-selective CK1 inhibitor (IC₅₀/[ATP] = 5 nM/32 µM, 40 nM/8 µM, and 251 nM/11 µM, respectively, in CK1γ2, CK1δ, and CK1α kinase assays), inhibiting GSK-3β only at much higher concentrations (IC₅₀ = 10.8 µM). Shown to suppress LRP6 phosphorylation in CK1γ2-/LRP6-expressing HEK293 transfectants both in cultures (IC₅₀ = 200 nM) in vitro and in mice (42% reduction 6 h post 50 mg/kg p.o.) in vivo.

A cell-permeable, ATP site-targeting, γ isotype-selective CK1 inhibitor (IC₅₀ = 5 nM).

Cell permeable: yes

Primary Target
CKIγ

Secondary Target
CKIδ

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

Huang, H., et al. 2012. ACS Med. Chem. Lett.3, 1059.

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

Toxicity: Standard Handling (A)