Chemical Name: 3-Chloro-N-[trans-4-(methylamino)cyclohexyl]-N-[[3-(4-pyridinyl)phenyl]methyl]benzo[b]thiophene-2-carboxamide
Biological ActivitySAG 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 nduces 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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A small molecule that binds Hedgehog and blocks its signaling in human cells.
Stanton et al.
Small molecule modulation of Smoothened activity.
Chen et al.
Small molecules greatly improve conversion of human-induced pluripotent stem cells to the neuronal lineage.
Mak et al.
Stem Cells Int., 2012;2012:140427
Citations for SAG
The citations listed below are publications that use Tocris products. Selected citations for SAG include:
5 Citations: Showing 1 - 5
Neuropathy-causing mutations in HSPB1 impair autophagy by disturbing the formation of SQSTM1/p62 bodies.
Authors: Haidar Et al.
Super-Obese Patient-Derived iPSC Hypothalamic Neurons Exhibit Obesogenic Signatures and Hormone Responses.
Authors: Rajamani Et al.
Cell Stem Cell 2018;22:698
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
Transcriptional comparison of human induced and primary midbrain DArgic neurons.
Authors: Xia Et al.
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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