| Chemical Properties | Back Directory | [Boiling point ]
793.0±60.0 °C(Predicted) | [density ]
1.53±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 100 mg/mL (172.92 mM) | [form ]
Solid | [pka]
4.01±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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) | [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]. | 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. |
| [References]
[1] Mahoney SJ, et al. A small molecule inhibitor of Rheb selectively targets mTORC1 signaling. Nat Commun. 2018 Feb 7;9(1):548. DOI:10.1038/s41467-018-03035-z |
|
|