
Rheb inhibitor NR1
CAS No. 2216763-38-9
Rheb inhibitor NR1( —— )
Catalog No. M33480 CAS No. 2216763-38-9
Rheb inhibitor NR1 is a selective mTORC1 inhibitor that suppresses the phosphorylation of T389pS6K1 and enhances the phosphorylation of S473pAKT.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 128 | Get Quote |
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5MG | 188 | Get Quote |
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10MG | 312 | Get Quote |
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25MG | 609 | Get Quote |
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50MG | 915 | Get Quote |
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100MG | 1512 | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameRheb inhibitor NR1
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NoteResearch use only, not for human use.
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Brief DescriptionRheb inhibitor NR1 is a selective mTORC1 inhibitor that suppresses the phosphorylation of T389pS6K1 and enhances the phosphorylation of S473pAKT.
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DescriptionRheb 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.(Rheb-IVK:Rheb-dependent mTORC1 kinase activity)
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In VitroCell Viability Assay Cell Line:Jurkat cells Concentration:1, 3 and 10 μM Incubation Time:48 h Result:Effectively reduced the size of Jurkat cells in a dose-dependent manner.Western Blot Analysis Cell Line:MCF-7, TRI102 and PC3 cells Concentration:0.37, 1.1, 3.3, 10 and 30 μM Incubation Time:90 min for MCF-7 and TRI102; 24 h for PC3 Result:Inhibited the phosphorylation of T389pS6K1 and increased the phosphorylation of S473pAKT in a dose-dependent manner.Western Blot Analysis Cell Line:MCF-7 Concentration:1, 3, 10 and 30 μM Incubation Time:2.5 h (then labeled the cells with an 35S-Met labeling mix for 30?min)Result:Dose-dependently reduced protein synthesis.
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In VivoAnimal Model:Male C57BL/6 mice (6-7 weeks; fast for 16 hours) 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.
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Synonyms——
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PathwayPI3K/Akt/mTOR signaling
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TargetmTOR
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RecptormTOR
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Research Area——
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Indication——
Chemical Information
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CAS Number2216763-38-9
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Formula Weight578.3
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Molecular FormulaC25H19BrCl2N2O3S
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 50 mg/mL (86.46 mM; Ultrasonic )
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SMILESCN(C)C(=O)c1ccc(Cn2c(cc3c(Br)cc(Sc4ccc(Cl)c(Cl)c4)cc23)C(O)=O)cc1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Mahoney SJ, et al. A small molecule inhibitor of Rheb selectively targets mTORC1 signaling. Nat Commun. 2018 Feb 7;9(1):548.?
molnova catalog



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