CC260 (CC-260) is a potent, selective inhitor of PI5P4Kα/β with Ki of 40/30 nM, respectively.
CC260 displays high selectivity against a panel of 396 protein kinases, modestly inhibits PIKfyve (Ki=200 nM), does not inhibit most PI3Ks, PI4Ks, or SphKs but modestly inhibits PI3K-γ (Ki ∼200 nM) and PI3K-δ (Ki ∼120 nM).
CC260 enhanced insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 but suppressed S6K phosphorylation by mTORC1, disrupted energy homeostasis in myotubes, selectively toxic toward p53-null tumor cells.
CC260 reduced tumor cell survival under nutrient stress.
