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CAS No. : 1258275-73-8
MCE 国际站:TMPA
产品活性:TMPA 是一种具有高亲和力的 Nur77 拮抗剂,与 Nur77 结合导致 LKB1 在细胞质中释放和穿梭,以激活 AMPKα。TMPA 能有效地降低血糖,减轻 II 型 db/db、高脂饮食和链脲霉素诱导的糖尿病小鼠的胰岛素抵抗。TMPA 能减少人类 T 细胞的 RICD,也可用于癌症和 T 细胞凋亡失调的研究。
研究领域:Epigenetics | PI3K/Akt/mTOR
作用靶点:AMPK
In Vitro: TMPA (5, 10, 20, 40, 80 μM; 6 h or 10 μM; 0.5, 1, 3, 6, 12, 24, 36, 48 h) antagonizes the Nur77-LKB1 interaction in a dose- and time-dependent manner in hepatic LO2 cells.
?TMPA (10 μM; 6 h) enhances the LKB1-AMPKα interaction but decreases the LKB1-Nur77 interaction under physio logical conditions in Lo2 cells.
?TMPA binds directly to LBD in specific conformation.
?TMPA (10, 20 μM; 6 h) induces LKB1 nuclear export to activate AMPKα in Lo2 cells.
?TMPA (10, 50, 100 μM; 4 h) impairs human T-cell RICD (restimulation-induced cell death).
In Vivo: TMPA (50 mg/kg; i.p.; single daily for 19 days) is capable of lowering blood glucose and improving glucose tolerance in type II diabetic mice.
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