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Cat.No. 3889 - GANT 58 | C24H16N4S | CAS No. 64048-12-0
Description: GLI1 antagonist; inhibits Hedgehog (Hh) signaling
Chemical Name: 2,3,4,5-Tetra(4-pyridyl)thiophene
Purity: ≥99% (HPLC)
Citations (1)

Biological Activity

GLI antagonist that inhibits GLI1-induced transcription (IC50 = 5 μM). Inhibits the hedgehog (Hh) signaling pathway downstream of SMO and SUFU causing GLI1 nuclear accumulation. Displays antiproliferative and antitumor activity in vivo.

Compound Libraries

GANT 58 is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 392.48
Formula C24H16N4S
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 64048-12-0
PubChem ID 253078
Smiles C1(C5=CC=NC=C5)=C(C3=CC=NC=C3)C(C2=CC=NC=C2)=C(C4=CC=NC=C4)S1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 9.81 25
ethanol 9.81 25

Preparing Stock Solutions

The following data is based on the product molecular weight 392.48. 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
0.25 mM 10.19 mL 50.96 mL 101.92 mL
1.25 mM 2.04 mL 10.19 mL 20.38 mL
2.5 mM 1.02 mL 5.1 mL 10.19 mL
12.5 mM 0.2 mL 1.02 mL 2.04 mL

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References are publications that support the biological activity of the product.

Lauth et al (2007) Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proc.Natl.Acad.Sci. 104 8455 PMID: 17494766

Beauchamp et al (2009) GLI1 is a direct transcriptional target of EWS-FLI1 oncoprotein. J.Biol.Chem. 284 9074 PMID: 19189974

Joo et al (2009) GLI1 is a central mediator of EWS/FLI1 signaling in Ewing tumors. PLoS ONE 4 7608 PMID: 19859563

If you know of a relevant reference for GANT 58, please let us know.

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1 Citation for GANT 58

Citations are publications that use Tocris products. Selected citations for GANT 58 include:

Oladapo (2017) Pharmacological targeting of GLI1 inhibits proliferation, tumor emboli formation and in vivo tumor growth of inflammatory breast cancer cells. Cancer Lett 411 136 PMID: 28965853

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