TMBIM6 inhibitor BIA is a specific inhibitor of TMBIM6 (BAX inhibitor-1, BI-1), prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, also suppresses ER release of Ca2+ from TMBIM6, has broad anticancer activities.
BIA decreases the binding between TMBIM6 and mTORC2 inhibits proliferation and cell viability of MCF7 and MDA-MB-231 cells highly expressed TMBIM6. BIA reduced cell proliferation by inducing the dissociation of TMBIM6 from mTORC2 and ribosome, result in cell death.
BIA suppresses ER release of Ca2+ from TMBIM6.
BIA decreases cell migration in HT1080, MCF7, MDA-MB-231, and SKBR3 cells, not TMBIM6 KO HT1080 cells.
BIA (1 mg/kg BIA, vehicle (0.1% DMSO with saline), 5 days per week during 25 days) markedly impaired cell-driven tumor growth in HT1080 and MDA-MB-231 xenograft mice.
TMBIM6, a member of the transmembrane BI-1 motif-containing family of proteins, is overexpressed in many cancer types.