GANT61 An antiproliferative Hh signaling pathway inhibitor

GANT61 (CAS 500579-04-4)

GANT61 | CAS 500579-04-4 is rated 5.0 out of 5 by 1.
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Synonym: 2,2'-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine
Application: An antiproliferative Hh signaling pathway inhibitor
CAS Number: 500579-04-4
Purity: >95%
Molecular Weight: 429.60
Molecular Formula: C27H35N5
* Refer to Certificate of Analysis for lot specific data (including water content).
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GANT61 is a cell-permeable hexahydropyrimidine compound, shown to be an inhibitor of GLI-mediated gene transactivation. GLI-mediated transcription is the final step in the Hedgehog (Hh) signaling pathway, therefore GANT61 halts hedgehog pathway effects. Sonic hedgehog, a homolog of Hedgehog is essential for proper embryonic development and the interference of GANT61 with its production could lead to potential developmental issues. Additionally, this compound was found to successfully inhibit proliferation of tumor cells in vitro in a GLI-dependent manner. GANT61 is an inhibitor of GLI-1 and GLI-2.


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. Guan, Cheng-Chao., et al., 2009. Sonic hedgehog alleviates the inhibitory effects of high glucose on the osteoblastic differentiation of bone marrow stromal cells. Bone. 45(6): 1146-52. PMID: 19683085
3. Stanton, Benjamin Z., et al., 2010. Small-molecule modulators of the Sonic Hedgehog signaling pathway. Molecular bioSystems. 6(1): 44-54. PMID: 20024066

Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml), ethanol (5 mg/ml), and 1:3 EtOH:PBS(PH 7.2) (0.25 mg/ml).
Storage :
Store at -20° C
Boiling Point :
549.00° C at 760 mmHg (Predicted)
Density :
1.14 g/cm3
Refractive Index :
n20D 1.63
IC50 :
inhibiting the transcripional activity of Gli1: IC50 = 5 µM; Zinc finger protein GLI1: IC50 = 40 µM (human); Sonic hedgehog protein: IC50 = 5 µM (Mus musculus)
pK Values :
pKb: 5.97
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
421610
MDL Number :
MFCD14635408
SMILES :
CN(C)C1=CC=CC=C1CN2CCCN(C2C3=CC=NC=C3)CC4=CC=CC=C4N(C)C

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GANT61  Product Citations

See how others have used GANT61. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 23757299  Zhu, G. et al. 2013. Oncol. Rep. 30: 904-10.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Srivastava Srivastava, RK. et al. (PubMed 25432075) found that GANT61, an inhibitor of GLI-mediated transcription, dampened the proliferation of both embryonal and alveolar rhabdomyosarcoma cells-derived xenograft tumors. It also significantly diminished AKT/mTOR signaling. -SCBT Publication Review
Date published: 2015-05-25
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