SMBA1

SMBA1 is an activator of Bax (K_i = 43.3 nM in a fluorescence polarization assay).¹ It selectively reduces viability in wild-type but not Bax^-/- mouse embryonic fibroblasts (MEFs) when used at a concentration of 25 µM. SMBA1 (5 µM) inhibits nicotine-induced increases in phosphorylated Bax levels in A549 lung cancer cells. It reduces viability in A549 cells when used at a concentration of 5 µM. SMBA1 (5, 10, or 15 µM) induces cell cycle arrest at the G₂/M phase in U87MG glioblastoma cells.² It disrupts the mitochondrial membrane potential in U87MG cells when used at a concentration of 15 µM. SMBA1 (5 or 10 µM) induces cytochrome c release from mitochondria and Bax insertion into mitochondrial membranes in A549 cells.¹ In vivo, SMBA1 (40 or 60 mg/kg per day) decreases tumor volume in an A549 mouse xenograft model.

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1. Xin, M., Li, R., Xie, M., et al. Small-molecule Bax agonists for cancer therapy. Nat. Commun. 5, 4935 (2014).

2. Fan, S., Xu, Q., Wang, L., et al. SMBA1, a Bax activator, induces cell cycle arrest and apoptosis in malignant glioma cells. Pharmacology 105(3-4), 164-172 (2020).