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)
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