iHAP1

iHAP1 (improved Heterocyclic Activator of PP2A 1) is a small molecule activator of protein phosphatase 2A (PP2A), a heterotrimeric serine/threonine phosphatase that functions as a critical tumor suppressor. PP2A is frequently inactivated in various malignancies, including colorectal cancer and melanoma, often through the overexpression of endogenous inhibitors or post-translational modifications. iHAP1 works by binding allosterically to the PP2A holoenzyme, thereby restoring its phosphatase activity and promoting the dephosphorylation of oncogenic substrates such as AKT, ERK, and MYC. In preclinical research, iHAP1 has demonstrated the ability to inhibit cell proliferation and induce apoptosis in cancer cell lines. It has also served as a structural template for the development of next-generation PP2A activators, such as PPA24 and PPA27, which aim to improve upon its potency and therapeutic profile.

Other names

improved Heterocyclic Activator of PP2A 1