Endovion is an orally active anion channel inhibitor. Endovion can specifically blocks VRAC/VSOAC channels and inhibits ANO1, thereby regulating cell volume and apoptotic signaling pathways. Endovion can be used in research related to pancreatic cancer and colorectal cancer[1-4].
In vitro, Endovion (0-800nM) was used to treat wild-type and H-ras-transformed NIH3T3 fibroblasts for 5 hours. Endovion significantly inhibited cell migration in a concentration-dependent manner[5]. Endovion (0.3-10μM) was simultaneously applied with interferon-γ to treat BV2 microglial cells for 16-18 hours. Endovion significantly inhibited nitric oxide production and inducible nitric oxide synthase expression[6].
References:
[1] Sørensen BH, Nielsen D, Thorsteinsdottir UA, et al. Downregulation of LRRC8A protects human ovarian and alveolar carcinoma cells against Cisplatin-induced expression of p53, MDM2, p21Waf1/Cip1, and Caspase-9/-3 activation. Am J Physiol Cell Physiol. 2016 Jun 1;310(11):C857-73.
[2] Hélix N, Strøbaek D, Dahl BH, et a. Inhibition of the endogenous volume-regulated anion channel (VRAC) in HEK293 cells by acidic di-aryl-ureas. J Membr Biol. 2003 Nov 15;196(2):83-94.
[3] Mao W, Wang Z, Wen S, et al. LRRC8A promotes Glaesserella parasuis cytolethal distending toxin-induced p53-dependent apoptosis in NPTr cells. Virulence. 2023 Dec;14(1):2287339.
[4] Pfeiffer A, Di Leo L, Bechmann MB, et al. Inhibition of ABCG2 by SCO-101 Enhances Chemotherapy Efficacy in Cancer. Int J Mol Sci. 2025 Apr 17;26(8):3790.
[5] Schneider L, Klausen TK, Stock C, et al. H-ras transformation sensitizes volume-activated anion channels and increases migratory activity of NIH3T3 fibroblasts. Pflugers Arch. 2008 Mar;455(6):1055-62.
[6] Kjaer K, Strøbaek D, Christophersen P, et al. Chloride channel blockers inhibit iNOS expression and NO production in IFNgamma-stimulated microglial BV2 cells. Brain Res. 2009 Jul 24;1281:15-24.