DX2-201

DX2-201 is a potent and selective oxidative phosphorylation (OXPHOS) complex I inhibitor with an IC50 of 312 nM. DX2-201 has anticancer effects[1].

Research Areas >> Cancer

IC50: 312 nM (OXPHOS complex I)[1]

DX2-201 (cmpound 2) potently inhibits the mitochondrial function by depleting ATP production in MIA PaCa-2 cells when glucose is replaced by galactose in the medium, a condition that forces mammalian cells to rely on OXPHOS[1]. DX2-201 depletes ATP production with an IC50 value of 118.5 nM in the galactose-containing medium[1]. DX2-201 significantly inhibits OXPHOS complex I as determined by its inhibition of oxidation of NADH to NAD+ in the NAD/NADH assay (IC50 = 312 nM)[1]. DX2-201 inhibits MIA PaCa-2 and BxPC-3 cells growth with IC50 values of 0.4 μM and 0.6 μM, respectively[1].

[1]. Ding Xue, et al. Discovery and Lead Optimization of Benzene-1,4-disulfonamides as Oxidative Phosphorylation Inhibitors.J Med Chem. 2022 Jan 13;65(1):343-368. https://pubmed.ncbi.nlm.nih.gov/34982568/