RRX-001是一種有效的葡萄糖-6-磷酸脫氫酶 (G6PD) 抑制劑。 RRX-001具有強(qiáng)抗瘧效果, 藥物敏感性測(cè)試表明, 抑制寄生蟲(chóng)活性IC50 = 0.14 ± 0.04 ug/ml。

RRx-001的生物活性

RRx-001 is a potent inhibitor of G6PD. RRx-001 shows potent antimalarial, although as a single agent, the drug sensitivity testing indicated that higher dose of RRx-001 was required to inhibited 50 % of the parasite's activity (IC50 = 0.14 ± 0.04 ug/ml).
IC50 value: 0.14 ± 0.04 ug/ml [1]
Target: G6PD
in vitro: RRx-001 is a novel, systemically non-toxic, epigenetic anticancer agent for multiple tumour types, with activity mediated through increased nitric oxide (NO) production and PPP inhibition. [1]
in vivo: RRx-001is a novel, nonexplosive molecule modified from a class of solid rocket propellants, has shown promise as a novel cancer therapeutic agent in a number of cell lines and tumor models. In mouse models, RRx-001 administered intravenously as a single agent was equipotent to cisplatin while better tolerated. RRx-001 also showed activity as a radiosensitizer in both in vitro and in vivo models. The activity of RRx-001 is thought to be associated with a nucleophilic substitution by circulating thiol compounds and covalent binding of RRx-001 to cysteinyl residues in Hb, followed by the generation of nitrogen oxides. [2]