GSK-3beta Inhibitor XXVII, CESI

A cell-permeable, 3-hydroxychromone derived compound that acts as a selective and reversible inhibitor of GSK-3β (IC₅₀<100 nM). Shown to increase phosphorylation at Ser9. Does not show any inhibitory effect on a panel of 15 other protein kinases, including AMPK and Akt. By blocking GSK-3β activity, it acts as a positive regulator of b-catenin signaling. Does not affect the viability or the growth rate of 3T3-L1 preadipocytes, however, it significantly reduces their differentiation into adipocytes (˜ 50 to 100 nM). Exerts anti-adipogenic activity by down-regulating C/EBPa and PPARg. Shown to reduce adipocyte size and diminish weight gain in diet-induced obese mice without affecting their daily food intake.

Cell permeable: yes

Primary Target
GSK3b

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

S. Lee et al. 2013, Biochemical Pharmacology85, 965.

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