GANT 58 An inhibitor of GLI1-induced transcription

GANT 58 (CAS 64048-12-0)

GANT 58 | CAS 64048-12-0 is rated 5.0 out of 5 by 1.
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Synonym: 2,3,4,5-Tetra(4-pyridyl)thiophene
Application: An inhibitor of GLI1-induced transcription
CAS Number: 64048-12-0
Purity: ≥98%
Molecular Weight: 392.48
Molecular Formula: C24H16N4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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GANT 58 is a GLI-1 and GLI-2 (GLI) antagonist and an inhibitor of GLI induced transcription. Reported to inhibit the hedgehog (Hh) signaling pathway downstream of SUFU and SMO thereby affecting GLI1 nuclear accumulation. It also displays antiproliferative and antitumor activity in vivo.


References

1. Lauth, Matthias., et al., 2007. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proceedings of the National Academy of Sciences of the United States of America. 104(20): 8455-60. PMID: 17494766
2. Beauchamp, Elspeth., et al., 2009. GLI1 is a direct transcriptional target of EWS-FLI1 oncoprotein. The Journal of biological chemistry. 284(14): 9074-82. PMID: 19189974
3. Joo, Jay., et al., 2009. GLI1 is a central mediator of EWS/FLI1 signaling in Ewing tumors. PloS one. 4(10): e7608. PMID: 19859563

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mM), and ethanol (25 mM).
Storage :
Store at 4° C
Melting Point :
256-258° C
Refractive Index :
n20D 1.66
IC50 :
GLI1-induced transcription: IC50 = 5 µM; Hedgehog signaling: IC50 = 5 µM (human); Sonic hedgehog protein: IC50 = 5 µM (mouse)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
253078
SMILES :
C1=CN=CC=C1C2=C(SC(=C2C3=CC=NC=C3)C4=CC=NC=C4)C5=CC=NC=C5

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Certificate of Analysis

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Rated 5 out of 5 by from Lauth et al Lauth et al. (PubMed ID 17494766) found that GANT 58 reduced tumor cell proliferation by reducing GLI1-mediated transcription and blocking Hedgehog signaling in HEK293 cells. -SCBT Publication Review
Date published: 2015-04-08
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