Rheb inhibitor NR1

製品番号: HY-124798 純度: 99.26%: Data Sheet SDS COA 取扱説明書
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Technical Support

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)}

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Rheb inhibitor NR1 構造式

CAS 番号 : 2216763-38-9

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 318	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 318	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$250	在庫あり	Estimated Time of Arrival: December 31
10 mg	$400	在庫あり	Estimated Time of Arrival: December 31
25 mg	$800	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1280	在庫あり	Estimated Time of Arrival: December 31
100 mg	$2050	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

顧客検証

mTOR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

mTOR mTORC1 mTORC2

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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^[1].
^{(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)}

IC₅₀ & Target

Rheb, mTORC1^[1]

体外実験

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 of ^T389pS6K1 and increases the phosphorylation of ^S473pAKT in MCF-7, TRI102 and PC3 cells^[1].
? NR1 (1-30 μM; 2.5 h) reduced protein synthesis in MCF-7^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 of ^T389pS6K1 and increased the phosphorylation of ^S473pAKT 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 an ³⁵S-Met labeling mix for 30 min)
Result:	Dose-dependently reduced protein synthesis.

体内実験

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^[1].

MedChemExpress (MCE) 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)^[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 for ^T37/464E-BP1 in skeletal muscle.

分子量

578.30

分子式

C₂₅H₁₉BrCl₂N₂O₃S

CAS 番号

2216763-38-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(C(N1CC2=CC=C(C(N(C)C)=O)C=C2)=CC3=C1C=C(SC4=CC=C(Cl)C(Cl)=C4)C=C3Br)O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (86.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.26%

Select Batch:

データシート (282 KB) SDS (393 KB)

COA (256 KB) HNMR (136 KB) RP-HPLC (249 KB) MS (162 KB)

取扱説明書 (2659 KB)

参考文献

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7292 mL	8.6460 mL	17.2921 mL	43.2302 mL
	5 mM	0.3458 mL	1.7292 mL	3.4584 mL	8.6460 mL
	10 mM	0.1729 mL	0.8646 mL	1.7292 mL	4.3230 mL
	15 mM	0.1153 mL	0.5764 mL	1.1528 mL	2.8820 mL
	20 mM	0.0865 mL	0.4323 mL	0.8646 mL	2.1615 mL
	25 mM	0.0692 mL	0.3458 mL	0.6917 mL	1.7292 mL
	30 mM	0.0576 mL	0.2882 mL	0.5764 mL	1.4410 mL
	40 mM	0.0432 mL	0.2162 mL	0.4323 mL	1.0808 mL
	50 mM	0.0346 mL	0.1729 mL	0.3458 mL	0.8646 mL
	60 mM	0.0288 mL	0.1441 mL	0.2882 mL	0.7205 mL
	80 mM	0.0216 mL	0.1081 mL	0.2162 mL	0.5404 mL