BioCentury
ARTICLE | Distillery Therapeutics

Cancer; autoimmune disease

March 20, 2018 11:10 PM UTC

In vitro, cell culture and mouse studies suggest inhibiting CDK9 and GSK3 could help treat cancer, Crohn’s disease and ulcerative colitis. Chemical synthesis and in vitro kinase inhibition assays of diaminothiazole analogs yielded a compound that inhibited CDK9, GSK3A and GSK3B activity with IC50 values of 321, 327 and 657 nM, respectively. In a total of seven human and mouse prostate, squamous cell carcinoma, melanoma, pancreatic and neuroblastoma cell lines, the compound decreased viability compared with vehicle. In mouse models of melanoma and pancreatic cancer, the compound decreased tumor volume. In mouse models of Crohn’s disease and ulcerative colitis, the compound decreased scores of disease severity. Next steps by Apogee Biotechnology Corp. could include optimizing and testing the inhibitor in additional models of cancer and IBD.

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