Rheb inhibitor NR1

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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。

Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1?μM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity. (Rheb-IVK:Rheb-dependent mTORC1 kinase activity)

Cell Viability Assay Cell Line:Jurkat cells Concentration:1, 3 and 10 μM Incubation Time:48 h Result:Effectively reduced the size of Jurkat cells in a dose-dependent manner.Western Blot Analysis Cell Line:MCF-7, TRI102 and PC3 cells Concentration:0.37, 1.1, 3.3, 10 and 30 μM Incubation Time:90 min for MCF-7 and TRI102; 24 h for PC3 Result:Inhibited the phosphorylation of T389pS6K1 and increased the phosphorylation of S473pAKT in a dose-dependent manner.Western Blot Analysis Cell Line:MCF-7 Concentration:1, 3, 10 and 30 μM Incubation Time:2.5 h (then labeled the cells with an 35S-Met labeling mix for 30?min)Result:Dose-dependently reduced protein synthesis.

Animal Model:Male C57BL/6 mice (6-7 weeks; fast for 16 hours) Dosage:30 mg/kg Administration:IP; single dosage Result:Sustained over 5?μM for 2?h.Significantly reduced 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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PI3K/Akt/mTOR signaling

mTOR

mTOR

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2216763-38-9

578.3

C25H19BrCl2N2O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (86.46 mM; 超声助溶 )

CN(C)C(=O)c1ccc(Cn2c(cc3c(Br)cc(Sc4ccc(Cl)c(Cl)c4)cc23)C(O)=O)cc1

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(-20℃)

With Ice Pack

≥ 2 years