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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Rheb inhibitor NR1
  • Note
    Research use only, not for human use.
  • Brief Description
    Rheb inhibitor NR1 is a selective mTORC1 inhibitor that suppresses the phosphorylation of T389pS6K1 and enhances the phosphorylation of S473pAKT.
  • Description
    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.(Rheb-IVK:Rheb-dependent mTORC1 kinase activity)
  • In Vitro
    Cell 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.
  • In Vivo
    Animal 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.
  • Synonyms
    ——
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    mTOR
  • Recptor
    mTOR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2216763-38-9
  • Formula Weight
    578.3
  • Molecular Formula
    C25H19BrCl2N2O3S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (86.46 mM; Ultrasonic )
  • SMILES
    CN(C)C(=O)c1ccc(Cn2c(cc3c(Br)cc(Sc4ccc(Cl)c(Cl)c4)cc23)C(O)=O)cc1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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.?
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