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Rheb inhibitor NR1

Chemical Structure : Rheb inhibitor NR1

CAS No.: 2216763-38-9

Rheb inhibitor NR1

Catalog No.: PC-62515Not For Human Use, Lab Use Only.

Rheb inhibitor NR1 is a small molecule that binds Rheb in the switch II domain (IC50=2.1 uM, Kd=1.5 uM) and selectively blocks mTORC1 signaling, potently inhibits mTORC1 driven phosphorylation of S6K1 but does not inhibit phosphorylation of AKT or ERK.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Rheb inhibitor NR1 is a small molecule that binds Rheb in the switch II domain (IC50=2.1 uM, Kd=1.5 uM) and selectively blocks mTORC1 signaling, potently inhibits mTORC1 driven phosphorylation of S6K1 but does not inhibit phosphorylation of AKT or ERK.
In contrast to rapamycin, NR1 does not cause inhibition of mTORC2 upon prolonged treatment, potently and selectively inhibits mTORC1 in mouse kidney and muscle in vivo.

Physicochemical Properties

M.Wt 578.302
Formula C25H19BrCl2N2O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-bromo-6-((3,4-dichlorophenyl)thio)-1-(4-(dimethylcarbamoyl)benzyl)-1H-indole-2-carboxylic acid

References

1. Mahoney SJ, et al. Nat Commun. 2018 Feb 7;9(1):548.

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