M190S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M190S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M190S has orally bioactivity with excellent brain permeability.
M190S (0.1-10000 nM, 24-48 h) inhibits apoptosis induced by Bax as well as Bak[1].M190S (0-10μM, 4 h) suppresses Staurosporine -induced apoptosis in MEFs [1].M190S (0-10μM, 24 h) inhibits Etoposide -induced apoptosis in Neuro2a cells[1].M190S (500 nM, 24 h) inhibits Obatoclax -induced apoptosis in ARPE19 cells[1].M190S (500 nM, 48 h) suppresses the conformation change (N-terminal exposure) and mitochondrial translocation of Bax[1].M190S (1.0 μM, 4h) decreases mitochondrial oxygen consumption and reactive oxygen species, whereas M190S (0.1-1 nM, 4 h) increases glycolysis[1].
M190S (10mg/kg p.o., three time in 48 h) protects the retina from the bright-light-induced photoreceptor death[1].M190S (1 mg/kg, i.p., i.v., 5 mg/kg, o.p. 10 mg/kg 1 time) is an orally bioactive cell death inhibitor penetrating blood-brain/retina-barrier[1].
References:
[1]. Mieko Matsuyama, et al. Development of novel cytoprotective small compounds inhibiting mitochondria-dependent cell death. Science 26, 107916, October 20, 2023