Rheb inhibitor NR1
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)
Product Specifications
CAS Number
[2216763-38-9]
UNSPSC
12352005
Hazard Statement
H302, H315, H319
Target
MTOR
Type
Reference compound
Related Pathways
PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer; Inflammation/Immunology; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/rheb-inhibitor-nr1.html
Concentration
10mM
Purity
99.26
Solubility
DMSO : 50 mg/mL (ultrasonic)
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
Molecular Formula
C25H19BrCl2N2O3S
Molecular Weight
578.30
Precautions
H302, H315, H319
References & Citations
[1]Mahoney SJ, et al. A small molecule inhibitor of Rheb selectively targets mTORC1 signaling. Nat Commun. 2018 Feb 7;9 (1) :548.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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