Description: Potent Smoothened (Smo) receptor antagonist Chemical Name: N-[[1-(2-Methoxyphenyl)-1H-indazol-5-yl]methyl]-2-propylpentanamide Purity: ≥98% (HPLC) Biological Activity Technical Data Solubility Calculators DatasheetsReferences

Biological Activity

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).

Compound Libraries

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Technical Data

M. Wt	379.5
Formula	C23H29N3O2
Storage	Store at +4°C
Purity	≥98% (HPLC)
PubChem ID	44250034
InChI Key	WATNXVHKRRTUFK-UHFFFAOYSA-N
Smiles	O=C(C(CCC)CCC)NCC1=CC=C(N(C3=CC=CC=C3OC)N=C2)C2=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM Solubility

DMSO	37.95	100
ethanol	37.95	100

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 solvent 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

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Product Datasheets

Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDS

References

References are publications that support the products\' biological activity.

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, supplier, M25, Smoothened, SMO, antagonists, inhibitors, inhibits, Hedgehog, signaling, pathway, SAG, Smoothened, Receptors, Hedgehog, Signaling, Smoothened, Receptors, Tocris Bioscience