Rheb inhibitor NR1,2216763-38-

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Rheb inhibitor NR1

CAS No. : 2216763-38-9

MCE 国际站：Rheb inhibitor NR1

产品活性：Rheb inhibitor NR1 是一种 Rheb 抑制剂，IC₅₀ 为 2.1 μM。Rheb inhibitor NR1 可直接结合 Rheb switch II 结构域，选择性抑制 mTORC1 的激活。Rheb inhibitor NR1 抑制 mTORC1 驱动的 ^T389pS6K1 的磷酸化，并以剂量依赖的方式增加 ^S473pAKT 的磷酸化。Rheb inhibitor NR1 不影响 mTORC2 的活性。

研究领域：PI3K/Akt/mTOR

作用靶点：mTOR

In Vitro: NR1 (1-10 μM; 48 h) reduces the size of Jurkat cells.
?NR1 (0.37-30 μM; 90 min for MCF-7 and TRI102; 24 h for PC3) inhibits the phosphorylation of ^T389pS6K1 and increases the phosphorylation of ^S473pAKT in MCF-7, TRI102 and PC3 cells.
?NR1 (1-30 μM; 2.5 h) reduced protein synthesis in MCF-7.

In Vivo: NR1 (30 mg/kg; IP; single dosage) significantly reduces mTORC1 activity in both kidney and skeletal muscle, and exhibited a clear band shift for ^T37/464E-BP1 in skeletal muscle.

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