My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    Smoothened Agonist (SAG)
    Smoothened Agonist (SAG)

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V1338
    CAS #: 912545-86-9Purity ≥98%

    Description: Smoothened Agonist (SAG), a benzothiophene analog, is a potent and cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells. SAG potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM). SAG induces pathway activation independently of Ptch proteins. The Smoothened receptor (SMO) mediates signal transduction in the hedgehog pathway, which is implicated in normal development and carcinogenesis. SMO antagonists can suppress the growth of some tumors. 

    References: Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6; Neurosci Lett. 2010 Sep 27;482(2):81-5.

    Related CAS #: 912545-86-9 (free base); 2095432-58-7 (HCl)   

    Customer Validation
    Top Publications Citing Invivochem Products
    • Citation of InvivoChem Vorinostat (V0255) by Nature 2021, 597(7874):119-125
    • Citation of InvivoChem Larotrectinib (V2599) by Cell. 2020 Nov 25;183(5):1202-1218.e25
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022: 8, eabm9427.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3
    • Citation of InvivoChem Larotrectinib (V2599) by Cell 2020, doi: 10.1016/j.cell.2020.10.016.
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022, doi: 10.1126/sciadv.abm9427.
    • Citation of InvivoChem Vorinostat/SAHA (V0255) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem Vitrakvi by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem APR-246 by Science Adv 2022, PMID: 36103522.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem LOXO-101 by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem Eprenetapopt by Science Adv 2022, PMID: 36103522.
    • Citation of InvivoChem Vorinostat/SAHA (V0255) by Nature 2021, PMID: 34433969
    • Citation of InvivoChem  ARRY-470 by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, PMID: 34433969
    • Citation of InvivoChem BMH-21 (V1435) by Cell Stem Cell 2020, 26(6): 845-861.e12.
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022, doi: 10.1126/sciadv.abm9427.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem V33339 Lys-SMCC-DM1 by PNAS Nexus 2022, pgac063, https://academic.oup.com/pna
    • Citation of InvivoChem 5-azacytidine by Nature 2021, PMID: 34433969
    • Citation of InvivoChem Ruxolitinib/Filgotinib/BMS-911543/Decernotinib by J Allergy Clin Immunol 2020
    • Citation of InvivoChem LGK974 /WNT974 (V1353) by  Cancer Cell 2021 Apr 12;39(4):529-547.e7.
    • Citation of InvivoChem V1386 Napabucasin (BBI-608) by J Exp Clin Cancer Res 2021 Oct 13;40(1):319.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem Epacadostat/INCB024360 (V0942) by Cancer Discov 2022: 12(4):1106-1127.
    • Citation of InvivoChem S63845 (V2797) by Cell Death and Disease 2020, 11:316.
    • Citation of InvivoChem BMS-582949 (V2668) by Cells 2020, 9(6):1472.
    • Citation of InvivoChem Apiin (V4467) by J Med Chem 2020, 63(15):8338-8358.
    • Citation of InvivoChem V0001 venetoclax by WO2021231323A1
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)490.06
    FormulaC28H28ClN3OS 
    CAS No.912545-86-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 71 mg/mL (134.8 mM)
    Water: N/A
    Ethanol: 40 mg/mL (75.9 mM)
    Other info

    Chemical Name: 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide

    SMILES Code: O=C(C1=C(Cl)C2=CC=CC=C2S1)N([[email protected]]3CC[[email protected]](NC)CC3)CC4=CC=CC(C5=CC=NC=C5)=C4 

    Exact Mass: 489.16416 

    Synonyms

    SAG free base; SAG; SAG (cyclopamine antagonist);SAG (Smo agonist)


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2
    In Vitro

    In vitro activity: SAG regulates Smo activity by binding directly to the Smo heptahelical bundle. SAG induces Smo-dependent signaling through Gli in a GRK2-dependent way. SAG also (1 nM) induces proliferation of neuronal and glial precursors without affecting the differentiation pattern of newly produced cells.


    Cell Assay: SAG acts downstream of Ptch1 in the Hh pathway and counteracts cyclopamine inhibition of Smo. SAG induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM and then inhibits expression at higher concentrations. In Smo-expressing Cos-1 cells, SAG yields an apparent dissociation constant (KD) of 59 nM for the SAG/Smo complex.

    In VivoIn the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities.
    Animal modelRats and mice
    Formulation & DosageRats: 2.5 nM, intracerebroventricular administration; Mice: 20 μg/g, i.p.
    References

    Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6; Neurosci Lett. 2010 Sep 27;482(2):81-5.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?