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.
PS432 (25 μM; 24 h) inhibits cancer cells proliferation, with IC50s of 30.7 μM (A549) and 12.4 μM (A427) in semi solid agar medium, for example[1].PS432 (50 μM; 12, 24, and 36 h) arrests cell cycle at G0/G1 phase in A549 lung cancer cells[1].
PS432 (2.5 mg/kg; i.p.; once daily for 14 d) inhibits tumor growth in xenograft model of lung cancer[1].
References:
[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.