Cat. No.: HY-124798

Rheb inhibitor NR1

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

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.

Purity: 99.26%
CAS No.: 2216763-38-9
Formula: C₂₅H₁₉BrCl₂N₂O₃S
Molecular Weight:578.30

Storage:

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

Rheb inhibitor NR1 Chemical Structure

CAS No.: 2216763-38-9

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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]

All mTOR Isoforms :

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.

Chemical Information

CAS No. 2216763-38-9
Appearance Solid
Molecular Weight 578.30
Formula C₂₅H₁₉BrCl₂N₂O₃S
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

Publications (3)

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Journal Impact Factor

Cell Death Dis

CRLF1 bridges AKT and mTORC2 through SIN1 to inhibit pyroptosis and enhance chemo-resistance in ovarian cancer. [Abstract]

2024 Sep 10;15(9):662. PMID: 39256356
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
PLoS Pathog

Picornavirus infection enhances aspartate by the SLC38A8 transporter to promote viral replication. [Abstract]

2023 Feb 3;19(2):e1011126. PMID: 36735752

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

Rheb inhibitor NR1

3 Cited Publications

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Rheb inhibitor NR1

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Publications Citing Use of MedChemExpress (MCE) Rheb inhibitor NR1

All mTOR Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Rheb inhibitor NR1 Related Classifications

HY-124798 Related Classifications