Kenpaullone

Kenpaullone is an ATP-competitive inhibitor of glycogen synthase kinase 3β (GSK-3β; Bain et al.; Leclerc et al.; Zaharevitz et al.). It inhibits GSK-3β, Cdk1/cyclin B, Cdk2/cyclin A, Cdk5/p25, and lymphocyte kinase with IC₅₀ values of 0.23, 0.4, 0.68, 0.85, and 0.47 µM, respectively (Bain et al.; Zaharevitz et al.).

REPROGRAMMING

• Replaces Klf4 in the generation of induced pluripotent stem (iPS) cells from mouse embryonic fibroblasts (MEFs) transduced with Oct4, Sox2, and c-Myc (Lyssiotis et al.).

DIFFERENTIATION

• Enhances neuronal differentiation in rat and human neural precursor cell cultures (Castelo-Branco et al.; Lange et al.).
• Promotes survival of motor neurons derived from mouse embryonic stem (ES) cells and from Amyotrophic Lateral Sclerosis (ALS) patient iPS cells (Yang et al.).

CANCER RESEARCH

• Inhibits KLF4 expression and self-renewal in breast cancer stem cells in vitro (Yu et al.).