Rheb inhibitor NR1_product_DataBase

Bioactivity

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)

Target

Rheb, mTORC1

Invitro

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]. Cell Viability Assay[1] Cell Line:

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:

Name

Rheb inhibitor NR1

CAS

2216763-38-9

Formula

C25H19BrCl2N2O3S

Molar Mass

578.30

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Mahoney SJ, et al. A small molecule inhibitor of Rheb selectively targets mTORC1 signaling. Nat Commun. 2018 Feb 7;9(1):548.

PeptideDB

Rheb inhibitor NR1

CAS: 2216763-38-9 F: C25H19BrCl2N2O3S W: 578.30