CRT-403

CRT-403 is a potent, selective, and ATP-competitive small molecule inhibitor of the Protein Kinase D (PKD) family, encompassing the isoforms PKD1, PKD2, and PKD3. Developed by Cancer Research Technology (the commercial arm of Cancer Research UK), the compound exhibits low nanomolar inhibitory activity (IC50 values of approximately 1 nM) across all three isoforms and demonstrates high selectivity against a broad panel of other kinases. PKD signaling is implicated in various pathological processes, including cardiac hypertrophy, inflammatory responses, and tumor progression. In oncology, PKD is known to regulate cell survival, DNA-mediated stress responses, and vascular endothelial growth factor (VEGF)-mediated angiogenesis. CRT-403 has been extensively used in preclinical research to validate PKD as a therapeutic target in cancers such as pancreatic and colorectal carcinoma, where it has demonstrated the ability to inhibit cell proliferation and induce apoptosis.

Other names

CRT403CRT-403CRT 403