Rheb inhibitor NR1|cas:2216763-38-9|西域试剂

Rheb inhibitor NR1,99.46%

产品编号：Bellancom-124798| CAS NO：2216763-38-9| 分子式：C₂₅H₁₉BrCl₂N₂O₃S| 分子量：578.30

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-124798	￥2500.00	杭州北京（现货）
Bellancom-124798	￥4000.00	杭州北京（现货）
Bellancom-124798	￥8000.00	杭州北京（现货）
Bellancom-124798	￥12800.00	杭州北京（现货）

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产品介绍

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 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)}

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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 for ^T37/464E-BP1 in skeletal muscle.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (86.46 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在西域网站选购。

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

参考文献

. Mahoney SJ, et al. A small molecule inhibitor of Rheb selectively targets mTORC1 signaling. Nat Commun. 2018 Feb 7;9(1):548. [Content Brief]

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