生物活性 | |||
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描述 | TMBIM6 is a Ca2+ channel-like protein that lowers the steady-state [Ca2+]ER. Overexpression of TMBIM6 promotes cancer metastasis by regulating cell mobility and invasiveness and glucose metabolism. TMBIM6 antagonist-1 is a potential TMBIM6 antagonist which prevents TMBIM6 binding to mTORC2, thus decreases mTORC2 activity, and it also regulates TMBIM6-leaky Ca2+. TMBIM6 antagonist-1 (BIA, 0.5-10 μM, 3 days) significantly and dose-dependently inhibited cell viability in HT1080, MCF7, MDA-MB-2341 and SKBR3 cells, with IC50 values of 1.7 ± 0.1 μM, 2.6 ± 0.4 μM, 2.6 ± 0.5 μM and 2.4 ± 0.4 μM, respectively. TMBIM6 antagonist-1 (BIA, 10 μM) treatment decreased cell migration in HT1080, MCF7, MDA-MB-231, and SKBR3 cells. In vivo, TMBIM6 antagonist-1 (1 mg/kg, IP 5 days per week during 25 days) significantly impaired cell-driven tumor growth in Six- to eight-week BklNbt:BALB/c/nu/nu old mice[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.73mL 0.75mL 0.37mL |
18.64mL 3.73mL 1.86mL |
37.28mL 7.46mL 3.73mL |
参考文献 |
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