TMBIM6 antagonist BIA (Bax inhibitor-1 antagonist, TMBIM6 antagonist-1) is a specific small molecule TMBIM6 (Bax inhibitor-1, BI-1) antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, also regulates TMBIM6-leaky Ca2+.
BIA inhibits proliferation and cell viability of MCF7 and MDA-MB-231 cells highly expressed TMBIM6 with IC50 of 1.7-2.6 uM.
BIA reduces cell proliferation by inducing the dissociation of TMBIM6 from mTORC2 and ribosome, result in cell death.
BIA suppresses ER release of Ca2+ from TMBIM6. decreased cell migration in HT1080, MCF7, MDA-MB-231, and SKBR3 cells, but not TMBIM6 KO HT1080 cells.
BIA ( 1 mg/kg, vehicle 0.1% DMSO with saline) markedly impaired cell-driven tumor growth of injected HT1080 and MDA-MB-231 cells into immunocompromised mice.
BIA significantly attenuated inflammatory cell infiltration, goblet cell hyperplasia, airway remodelling and Th2-associated cytokine expression in the lungs of A. fumigatus-challenged mice.
Transmembrane B cell lymphoma 2-associated X protein (BAX) inhibitor motif-containing (TMBIM)6, an inhibitor of ER stress.
TMBIM6 is a Ca2+ channel-like protein that lowers the steady-state [Ca2+]ER, which is expressed in the endoplasmic reticulum (ER) membrane surface.
TMBIM6 is overexpressed in many cancer types.