SAG

Catalog # Availability Size / Price Qty
4366/1
4366/10
SAG | CAS No. 912545-86-9 | Smoothened Receptor Agonists
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Description: Potent Smoothened receptor agonist; activates the Hedgehog signaling pathway

Chemical Name: 3-Chloro-N-[trans-4-(methylamino)cyclohexyl]-N-[[3-(4-pyridinyl)phenyl]methyl]benzo[b]thiophene-2-carboxamide

Purity: ≥98%

Product Details
Citations (21)
Supplemental Products
Reviews

Biological Activity

SAG is a potent Smoothened (Smo) receptor agonist (Kd = 59 nM); antagonizes Cyclopamine (Cat. No. 1623) action at the Smo receptor. SAG potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM) and induces pathway activation independently of Ptch proteins. SAG is a putative inhibitor of a cellular component required for Hedgehog signaling and also enhances neuronal differentiation of iPSCs into dopaminergic neurons.

SAG dihydrochloride (Cat. No. 6390) also available.

Technical Data

M.Wt:
490.06
Formula:
C28H28ClN3OS
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
912545-86-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Differentiation of Human Pluripotent Stem Cells into Colonic Organoids via Transient Activation of BMP Signaling
    JO Múnera, N Sundaram, SA Rankin, D Hill, C Watson, M Mahe, JE Vallance, NF Shroyer, KL Sinagoga, A Zarzoso-La, JR Hudson, JC Howell, P Chatuvedi, JR Spence, JM Shannon, AM Zorn, MA Helmrath, JM Wells
    Cell Stem Cell, 2017;0(0):.
  2. A small molecule that binds Hedgehog and blocks its signaling in human cells.
    Stanton et al.
    Nat.Chem.Biol., 2009;5:154
  3. Small molecule modulation of Smoothened activity.
    Chen et al.
    Proc.Natl.Acad.Sci.USA., 2002;99:14071
  4. Small molecules greatly improve conversion of human-induced pluripotent stem cells to the neuronal lineage.
    Mak et al.
    Stem Cells Int., 2012;2012:140427

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Citations for SAG

The citations listed below are publications that use Tocris products. Selected citations for SAG include:

21 Citations: Showing 1 - 10

  1. In vitro reconstitution of epigenetic reprogramming in the human germ line.
    Authors: Murase Et al.
    Nature  2024;
  2. Characterizing the Neuron-Glial Interactions by the Co-cultures of Human iPSC-Derived Oligodendroglia and Neurons.
    Authors: Xin Et al.
    Methods Mol Biol  2023;2683:103-111
  3. Primary cilia on muscle stem cells are critical to maintain regenerative capacity and are lost during aging.
    Authors: Aaron C Et al.
    Nat Commun  2022;13:1439
  4. Resolving cell state in iPSC-derived human neural samples with multiplexed fluorescence imaging.
    Authors: Beth A Et al.
    Commun Biol  2021;4:786
  5. A weakened interface in the P182L variant of HSP27 associated with severe Charcot-Marie-Tooth neuropathy causes aberrant binding to interacting proteins.
    Authors: John M Et al.
    EMBO J  2021;40:e103811
  6. Human Pluripotent Stem Cells for High-Throughput Drug Screening and Characterization of Small Molecules.
    Authors: Ruili Et al.
    Methods Mol Biol  2021;2454:811-827
  7. In Vitro Generation of Posterior Motor Neurons from Human Pluripotent Stem Cells.
    Authors: Anestis Et al.
    Curr Protoc  2021;1:e244
  8. Induced pluripotent stem cell-derived motor neurons of CMT type 2 patients reveal progressive mitochondrial dysfunction.
    Authors: Ludo Et al.
    Brain  2021;144:2471-2485
  9. SEM/FIB Imaging for Studying Neural Interfaces.
    Authors: Amos Et al.
    Dev Neurobiol  2020;80:305-315
  10. Electrophysiologic Characterization of Developing Human Embryonic Stem Cell-Derived Photoreceptor Precursors.
    Authors: Alon Et al.
    Invest Ophthalmol Vis Sci  2020;61:44
  11. Detailed Phenotyping and Therapeutic Strategies for Intronic ABCA4 Variants in Stargardt Disease.
    Authors: Carel B Et al.
    Mol Ther Nucleic Acids  2020;21:412-427
  12. Nek2 kinase displaces distal appendages from the mother centriole prior to mitosis.
    Authors: Shoji Et al.
    J Cell Biol  2020;219
  13. Aberrant interaction of FUS with the U1 snRNA provides a molecular mechanism of FUS induced amyotrophic lateral sclerosis.
    Authors: Frédéric H-T Et al.
    Nat Commun  2020;11:6341
  14. Generation of Human Neurons and Oligodendrocytes from Pluripotent Stem Cells for Modeling Neuron-Oligodendrocyte Interactions.
    Authors: Sundari Et al.
    J Vis Exp  2020;
  15. Axon-seq for in Depth Analysis of the RNA Content of Neuronal Processes.
    Authors: Eva Et al.
    Bio Protoc  2019;9:e3312
  16. Trehalose induces autophagy via lysosomal-mediated TFEB activation in models of motoneuron degeneration.
    Authors: Massimiliano Et al.
    Autophagy  2019;15:631-651
  17. Neuropathy-causing mutations in HSPB1 impair autophagy by disturbing the formation of SQSTM1/p62 bodies.
    Authors: Haidar Et al.
    Autophagy  2019;15:1051
  18. Super-Obese Patient-Derived iPSC Hypothalamic Neurons Exhibit Obesogenic Signatures and Hormone Responses.
    Authors: Rajamani Et al.
    Cell Stem Cell  2018;22:698
  19. Drug Screening Identifies Sigma-1-Receptor as a Target for the Therapy of VWM Leukodystrophy.
    Authors: Atzmon Et al.
    Front Mol Neurosci  2018;11:336
  20. Transcriptional comparison of human induced and primary midbrain DArgic neurons.
    Authors: Xia Et al.
    Sci.Rep.  2016;6:20270
  21. Accumulation of the Vitamin D Precursor Cholecalciferol Antagonizes Hedgehog Signaling to Impair Hemogenic Endothelium Formation.
    Authors: Cortes Et al.
    Nat Chem Biol  2015;5:471

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