PS432 is an allosteric inhibitor of atypical PKCs. It has been shown to target the PIF-pocket and significantly reduce tumor growth without side effects in mouse xenograft model.
PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models[1].
PS432 (2.5 mg/kg; i.p.; once daily for 14 d) inhibits tumor growth in xenograft model of lung cancer[1].
PKCζ: 18.5 μM (IC50); PKCι: 16.9 μM (IC50)
[1] Arencibia JM, et al. An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms. ACS Chem Biol. 2017 Feb 17;12(2):564-573. DOI:
10.1021/acschembio.6b00827
