Hh/Gli Antagonist, GANT58A cell-permeable tetrapyridinylthiophene

Hh/Gli Antagonist, GANT58 (CAS 64048-12-0)

Hh/Gli Antagonist, GANT58 is rated 5.0 out of 5 by 1.
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Application: A cell-permeable tetrapyridinylthiophene
CAS Number: 64048-12-0
Molecular Weight: 392.5
Molecular Formula: C24H16N4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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Hh/Gli Antagonist, GANT58 is a cell-permeable tetrapyridinylthiophene compound that acts as downstream Hedgehog (Hh) pathway blocker and targets Gli-mediated gene transactivation (IC50 ~ 5 7µM in SAG-stimulated Shh-L2 cells). Hh/Gli Antagonist, GANT58 has beem shown to reduce cellular mRNA levels of hedgehog target genes, Gli1, Hip1,& Ptch, and inhibit Gli-dependent tumor growth in vitro. Its action appears to be hedgehog pathway-selective, downstream of Smo and Sufu, but does not seem to interfere with Gli DNA binding. Hh/Gli Antagonist, GANT58 is an inhibitor of hedgehog.


References

Lauth, M., et al. 2007. Proc. Natl. Acad. Sci. USA 104, 8455.

Physical State :
Solid
Solubility :
Soluble in DMSO (>10 mg/mL), and ethanol (25 mM).
Storage :
Store at 4° C
Melting Point :
256-258° C
Boiling Point :
414.09° C at 760 mmHg (Predicted)
Density :
1.25 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
IC50 :
Gli-mediated gene transactivation: IC50 = ~ 5 µM (SAG-stimulated Shh-L2 cells); Sonic hedgehog protein: IC50 = 5 µM (mouse)
pK Values :
pKb: 4.50 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
253078
MDL Number :
MFCD01103196
SMILES :
C1=CN=CC=C1C2=C(SC(=C2C3=CC=NC=C3)C4=CC=NC=C4)C5=CC=NC=C5

Download SDS (MSDS)

Certificate of Analysis

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Hh/Gli Antagonist, GANT58  Product Citations

See how others have used Hh/Gli Antagonist, GANT58. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 21816948  Li, B. et al. 2011. Hum Mol Genet. -.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Hou Hou, X. et al. (PubMed 24394624) reported that inhibition of hedgehog signaling by GANT58 induces apoptosis and shows synergistic antitumor activity with AKT inhibitor in acute T cell leukemia cells. -SCBT Publication Review
Date published: 2015-06-03
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