Kenpaullone is an inhibitor of GSK-3β, HGK, and CDKs that exhibits anti-inflammatory, immunomodulatory, and neuroprotective activities. Kenpaullone increases levels of SREBP-1 as well as GIRK-4 and acetylcholine-activated inwardly rectifying K+ (IKACh) channels in diabetic mice. Kenpaullone also inhibits TGF-β-induced induction of RORγt and increases expression of Foxp3 in T cells, inhibiting pathology of experimental autoimmune encephalitis (EAE) in vivo. In pluripotent stem cells derived from autotrophic lateral sclerosis (ALS) patients, kenpaullone improves motor neuron survival. Additionally, this compound inhibits MPP+-induced cell death in cellular models of Parkinson’s disease by preventing changes in the mitochondrial membrane potential and inhibiting activation of caspases.