Actuate Therapeutics is developing novel therapeutics that target Glycogen Synthase Kinase-3β (GSK-3β). Activity and overexpression of GSK-3β have been implicated in many conditions, including cancer, Alzheimer’s disease, bipolar disorder, diabetes mellitus type II, and inflammatory conditions leading to fibrosis. GSK-3β is a novel and important target for the development of a new class of drugs that will have a significant impact on the treatment of cancer and select inflammatory diseases. In cancer, GSK-3β is heavily implicated in chemo- and radioresistance in tumor cells. Notably, aberrant nuclear accumulation of GSK-3β is a specific marker of malignant cells, but not of benign cells, making development of targeted therapies for GSK-3β an important and viable approach for cancer treatment.