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。
| 生物活性 | Rheb inhibitor NR1 is aRhebinhibitor with anIC50of 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 ofmechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation ofmTORC1drivenT389pS6K1 and increases the phosphorylation ofS473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influencemTORC2activity[1].
(Rheb-IVK: Rheb-dependentmTORC1kinase activity) |
| IC50& Target | |
体外研究
(In Vitro) | NR1 (1-10 μM; 48 h) reduces the size of Jurkat cells[1].
NR1 (0.37-30 μM; 90 min for MCF-7 and TRI102; 24 h for PC3) inhibits the phosphorylation ofT389pS6K1 and increases the phosphorylation ofS473pAKT in MCF-7, TRI102 and PC3 cells[1].
NR1 (1-30 μM; 2.5 h) reduced protein synthesis in MCF-7[1].
Cell Viability Assay[1] | 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[1] | 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 ofT389pS6K1 and increased the phosphorylation ofS473pAKT in a dose-dependent manner. |
Western Blot Analysis[1] | Cell Line: | MCF-7 | | Concentration: | 1, 3, 10 and 30 μM | | Incubation Time: | 2.5 h (then labeled the cells with an35S-Met labeling mix for 30 min) | | Result: | Dose-dependently reduced protein synthesis. |
|
体内研究
(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 forT37/464E-BP1 in skeletal muscle[1].
| Animal Model: | Male C57BL/6 mice (6-7 weeks; fast for 16 hours)[1] | | 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 forT37/464E-BP1 in skeletal muscle. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(86.46 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.7292 mL | 8.6460 mL | 17.2921 mL | | 5 mM | 0.3458 mL | 1.7292 mL | 3.4584 mL | | 10 mM | 0.1729 mL | 0.8646 mL | 1.7292 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.32 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.32 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com