Rheb inhibitor NR1
CAS No. : 2216763-38-9
| Size | Price | Stock |
|---|---|---|
| 5mg | $250 | In-stock |
| 10mg | $400 | In-stock |
| 25mg | $800 | In-stock |
| 50mg | $1280 | In-stock |
| 100mg | $2050 | In-stock |
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| Cat. No. : | HY-124798 |
| M.Wt: | 578.30 |
| Formula: | C25H19BrCl2N2O3S |
| Purity: | >98 % |
| Solubility: | DMSO : 50 mg/mL (ultrasonic) |
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].
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].
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