A Rheb inhibitor
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Rheb Inhibitor NR1

Item No. 43360

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-bromo-6-[(3,4-dichlorophenyl)thio]-1-[[4-[(dimethylamino)carbonyl]phenyl]methyl]-1H-indole-2-carboxylic acid
CAS Number
2216763-38-9
Molecular Formula
C25H19BrCl2N2O3S
Formula Weight
578.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(C1=CC2=C(N1CC3=CC=C(C(N(C)C)=O)C=C3)C=C(SC4=CC=C(C(Cl)=C4)Cl)C=C2Br)O
InChi Code
InChI=1S/C25H19BrCl2N2O3S/c1-29(2)24(31)15-5-3-14(4-6-15)13-30-22-11-17(34-16-7-8-20(27)21(28)10-16)9-19(26)18(22)12-23(30)25(32)33/h3-12H,13H2,1-2H3,(H,32,33)
InChi Key
MJYFVDNMTKLGTH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $440

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    25 mg

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    Product Description

    Rheb inhibitor NR1 is an inhibitor of Ras homolog enriched in brain (Rheb).1 It inhibits Rheb-dependent mTORC1 activity (IC50 = 2.1 µM). It selectively inhibits Rheb-depedent mTORC1 activity over Rheb-independent mTORC1 activity, mTORC2, Ras, and Rap1 at 30 µM. Rheb inhibitor NR1 (10 µM) decreases the size of Jurkat T cells and inhibits protein synthesis in MCF-7 breast cancer cells. In vivo, Rheb inhibitor NR1 (30 mg/kg) inhibits the phosphorylation of the mTORC1 substrates S6 and 4E-BP1 in mouse skeletal muscle and kidneys.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mahoney, S.J., Narayan, S., Molz, L., et al. A small molecule inhibitor of Rheb selectively targets mTORC1 signaling. Nat. Commun. 9(1), 548 (2018).