Rheb inhibitor NR1

Cat. No.: HY-124798 Purity: 99.46%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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)}

For research use only. We do not sell to patients.

Rheb inhibitor NR1 Chemical Structure

CAS No. : 2216763-38-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 275	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 275	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1280	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2050	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Rheb inhibitor NR1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All mTOR Isoform Specific Products:

View All Isoforms

mTOR mTORC1 mTORC2

Biological Activity
Purity & Documentation
References
Customer Review

Description

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]

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 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.

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^[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.

Molecular Weight

578.30

Formula

C₂₅H₁₉BrCl₂N₂O₃S

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Purity & Documentation

Purity: 99.46%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (256 KB) HNMR (132 KB) RP-HPLC (168 KB)

Handling Instructions (2659 KB)

References

[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