DT-061

DT-061 is a small molecule activator of protein phosphatase 2A (PP2A), a major serine/threonine phosphatase that acts as a tumor suppressor by dephosphorylating key oncogenic proteins such as MYC, AKT, and ERK. DT-061 belongs to a class of compounds known as Small Molecule Activators of PP2A (SMAPs). It specifically stabilizes the heterotrimeric PP2A holoenzyme containing the B56α regulatory subunit by binding to the interface of the A (scaffold) and C (catalytic) subunits. In preclinical studies, DT-061 has shown efficacy in various cancers, including KRAS-mutant lung cancer, triple-negative breast cancer, and myeloid neoplasias. In the context of -7/del7q myeloid neoplasia, it is being investigated for its ability to inhibit cell proliferation in cells with low expression of tumor suppressor phosphatases like PTPN12, suggesting that PP2A activation may compensate for the loss of other phosphatase-mediated tumor suppression.

Other names

SMAP DT-061