IACS-010759 是一种口服有效的线粒体氧化磷酸化复合体 I (OXPHOS) 抑制剂。IACS-010759 抑制增殖并诱导 OXPHOS 依赖性脑癌和急性髓性白血病 (AML) 模型中的凋亡。IACS-010759 在复发/难治性 AML 和实体瘤研究中具有潜力。

VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation, potentiated the effect of radiation in tumor spheroids in a synergistic manner. VLX600 is preferentially active against quiescent cells in colon cancer 3-D microtissues. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation and displays tumour growth inhibition in vivo.

IACS-010759 or IACS-10759 is a potent inhibitor of complex I of OXPHOS. IACS-10759 effectively inhibits ATP production and oxygen consumption in isolated mitochondria, and inhibits the conversion of NADH to NAD+ in immunoprecipitated complex I in low nM range. IACS-10759 is orally bioavailable with excellent physicochemical properties in preclinical species, and shows significant efficacy in multiple tumor indications both in vitro and in vivo. IACS-10759 causes robust tumor regression, but has no effect in the same model when glycolysis is restored.

S-Gboxin is an oxidative phosphorylation inhibitor that targets glioblastoma.