TMBIM6 antagonist-1

TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca2+[1].

Signaling Pathways >> PI3K/Akt/mTOR >> mTOR

Research Areas >> Cancer

TMBIM6 antagonist-1 (BIA, 0.5-10 μM, 3 days) significantly and dose-dependently inhibits cell viability in HT1080, MCF7, MDA-MB-2341 and SKBR3 cells, with IC50 values of 1.7 ± 0.1 μM for HT1080, 2.6 ± 0.4 μM for MCF cells, 2.6 ± 0.5 μM for MDA-MB-231 cells, and 2.4 ± 0.4 μM for SKBR3 cells, respectively[1]. TMBIM6 antagonist-1 (BIA, 10 μM) treatment decreases cell migration in HT1080, MCF7, MDA-MB-231, and SKBR3 cells, not TMBIM6 KO HT1080 cells[1]. Cell Viability Assay[1] Cell Line: HT1080, MCF7, MDA-MB-2341 and SKBR3 cells. Concentration: 0.5-10 μM. Incubation Time: 3 days. Result: Inhibited cell viability. Western Blot Analysis[1] Cell Line: WT and TMBIM6 KO HT1080 cells. Concentration: 0, 2, 5 μM. Incubation Time: Result: Downregulated the protein levels of AKT-pS473.

TMBIM6 antagonist-1 (1 mg/kg, IP 5 days per week during 25 days) significantly impaires cell-driven tumor growth[1]. Animal Model: Six- to eight-week BklNbt:BALB/c/nu/nu old mice (HT1080 and MDA-MB-231 cells)[1]. Dosage: 1 mg/kg. Administration: IP 5 days per week during 25 days. Result: Impaired cell-driven tumor growth.

[1]. Hyun-Kyoung Kim, et al. TMBIM6/BI-1 contributes to cancer progression through assembly with mTORC2 and AKT activation. Nat Commun. 2020 Aug 11;11(1):4012.