AKOS-22

AKOS-22 is a potent mitochondrial protein VDAC1 (voltage-dependent anion channel 1) inhibitor (Kd=15.4 μM). AKOS-22 interacts with VDAC1 and inhibiting both VDAC1 oligomerization and apoptosis. AKOS-22 protects against mitochondrial dysfunction[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Research Areas >> Neurological Disease

Kd: 15.4 μM (VDAC1)[1]

AKOS-22 (5-20 μM; 2 hours) inhibits both VDAC1 oligomerization and apoptosis in a concentration-dependent manner (IC50=7.5 μM)[1]. AKOS-22 inhibits selenite-induced VDAC1 oligomerization, Cyto c release and apoptosis in HEK-293 cells (IC50=3.3-3.6 μM). AKOS-22 (30 μM, 2 h) inhibits cisplatin-induced VDAC1 oligomerization and apoptosis in neuroblastoma cell line SH-SY5Y. AKOS-22 prevents the elevation of [Ca2+]I associated with apoptosis induction, and thus Ca2+ accumulation by the mitochondria[1].

[1]. Ben-Hail D, et al. Novel Compounds Targeting the Mitochondrial Protein VDAC1 Inhibit Apoptosis and Protectagainst Mitochondrial Dysfunction. Biol Chem. 2016 Nov 25;291(48):24986-25003.