Rheb inhibitor NR1 is a Rheb inhibitor with an IC 50 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 T389 pS6K1 and increases the phosphorylation of S473 pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity (Rheb-IVK: Rheb-dependent mTORC1 kinase activity) In Vitro NR1 (1-10 μM; 48 h) reduces the size of Jurkat cells. NR1 (0.37-30 μM; 90 min for MCF-7 and TRI102; 24 h for PC3) inhibits the phosphorylation of T389 pS6K1 and increases the phosphorylation of S473 pAKT in MCF-7, TRI102 and PC3 cells. NR1 (1-30 μM; 2.5 h) reduced protein synthesis in MCF-7. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell 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 T389 pS6K1 and increased the phosphorylation of S473 pAKT in a dose-dependent manner. Western Blot AnalysisCell Line: MCF-7 Concentration: 1, 3, 10 and 30 μM Incubation Time: 2.5 h (then labeled the cells with an 35 S-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 T37/46 4E-BP1 in skeletal muscle . 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) 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 T37/46 4E-BP1 in skeletal muscle. Form:Solid IC50& Target:Rheb, mTORC1
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
Rheb inhibitor NR1
CAS number：2216763-38-9 molecular formula：C25H19BrCl2N2O3S
overview
compound introduction
Specs
| Chinese alias | Rheb 抑制剂 NR1 | ||
| English alias | DTXSID201336670 | US11339144, Compound I-102 | Rheb inhibitor NR1 | 4-Bromo-6-[(3,4-dichlorophenyl)thio]-1-[[4-[(dimethylamino)carbonyl]phenyl]methyl]-1H-indole-2-carboxylic acid | AKOS040742547 | UNII-N6P39EU2QU | HY124798 | HY-124798 | N6P39EU2QU | 1H-I | ||
| CAS number | 2216763-38-9 | molecular formula | C25H19BrCl2N2O3S |
| molecular weight | 578.30 g/mol | Exact mass | ≥99% |
| PSA | 87.800 Ų | logp | 6.900 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
