For research use only. Not for therapeutic Use.
Rheb Inhibitor NR1(CAT: I017622) is a selective small-molecule inhibitor of Rheb with an IC₅₀ of 2.1 μM in the Rheb-IVK assay. It binds directly to the switch II domain of Rheb, preventing activation of mTORC1 without affecting mTORC2. NR1 suppresses phosphorylation of the mTORC1 substrate T389pS6K1 while enhancing phosphorylation of S473pAKT in a dose-dependent manner. In cellular models (MCF-7, TRI102, PC3), NR1 reduces protein synthesis and cell size, while in vivo (30 mg/kg, i.p.) it significantly decreases mTORC1 activity in kidney and skeletal muscle. NR1 is a valuable probe for studying Rheb-mediated signaling and therapeutic targeting of mTORC1.
| CAS Number | 2216763-38-9 |
| Synonyms | 4-bromo-6-(3,4-dichlorophenyl)sulfanyl-1-[[4-(dimethylcarbamoyl)phenyl]methyl]indole-2-carboxylic acid |
| Molecular Formula | C25H19BrCl2N2O3S |
| Purity | ≥95% |
| IUPAC Name | 4-bromo-6-(3,4-dichlorophenyl)sulfanyl-1-[[4-(dimethylcarbamoyl)phenyl]methyl]indole-2-carboxylic acid |
| InChI | InChI=1S/C25H19BrCl2N2O3S/c1-29(2)24(31)15-5-3-14(4-6-15)13-30-22-11-17(34-16-7-8-20(27)21(28)10-16)9-19(26)18(22)12-23(30)25(32)33/h3-12H,13H2,1-2H3,(H,32,33) |
| InChIKey | MJYFVDNMTKLGTH-UHFFFAOYSA-N |
| SMILES | CN(C)C(=O)C1=CC=C(C=C1)CN2C(=CC3=C2C=C(C=C3Br)SC4=CC(=C(C=C4)Cl)Cl)C(=O)O |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
