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Potent Smoothened (Smo) receptor antagonist (IC50 = 5 nM). Inhibits the Hedgehog signaling pathway. Inhibits Shh induced Gli luciferase reporter activity in Shh-light 2 cells (IC50 = 5 nM). Antagonizes GSA-10 and SAG-mediated differentiation of the C3H10T1/2 cell line (IC50 values are 69 and 115 nM, respectively).
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 379.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.64 mL||13.18 mL||26.35 mL|
|5 mM||0.53 mL||2.64 mL||5.27 mL|
|10 mM||0.26 mL||1.32 mL||2.64 mL|
|50 mM||0.05 mL||0.26 mL||0.53 mL|
References are publications that support the biological activity of the product.
Dessole et al (2009) Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway. Bioorg.Med.Chem.Lett. 19 4191 PMID: 19540115
Gorojankina et al (2013) Discovery, molecular and pharmacological characterization of GSA-10, a novel small-molecule positive modulator of Smoothened. Mol.Pharmacol. 83 1020 PMID: 23448715
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Keywords: M 25, M 25 supplier, M25, Smoothened, SMO, antagonists, inhibitors, inhibits, Hedgehog, signaling, pathway, SAG, Receptors, Signaling, 4917, Tocris Bioscience
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