GANT-61 - CAS 500579-04-4
Catalog number:
B0084-272119
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C27H35N5
Molecular Weight:
429.612
COA:
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Targets:
Gli
Description:
GANT 61 is a GLI antagonist that inhibits GLI1 activation of gene expression with an IC50 value of 5 μM.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-272119 100 mg $399 In stock
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Brife Description:
GLI antagonist
Synonyms:
2-[[3-[[2-(dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline
MSDS:
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InChIKey:
KVQOGDQTWWCZFX-UHFFFAOYSA-N
InChI:
InChI=1S/C27H35N5/c1-29(2)25-12-7-5-10-23(25)20-31-18-9-19-32(27(31)22-14-16-28-17-15-22)21-24-11-6-8-13-26(24)30(3)4/h5-8,10-17,27H,9,18-21H2,1-4H3
Canonical SMILES:
CN(C)C1=CC=CC=C1CN2CCCN(C2C3=CC=NC=C3)CC4=CC=CC=C4N(C)C
1.In vitro and in vivo inhibition of breast cancer cell growth by targeting the Hedgehog/GLI pathway with SMO (GDC-0449) or GLI (GANT-61) inhibitors.
Benvenuto M1, Masuelli L2, De Smaele E2, Fantini M1, Mattera R1,3, Cucchi D3, Bonanno E4, Di Stefano E2, Frajese GV5, Orlandi A4, Screpanti I3, Gulino A3, Modesti A1, Bei R1. Oncotarget. 2016 Feb 23;7(8):9250-70. doi: 10.18632/oncotarget.7062.
Aberrant Hedgehog (Hh)/glioma-associated oncogene (GLI) signaling has been implicated in cancer progression. Here, we analyzed GLI1, Sonic Hedgehog (Shh) and NF-κB expression in 51 breast cancer (ductal carcinoma) tissues using immunohistochemistry. We found a positive correlation between nuclear GLI1 expression and tumor grade in ductal carcinoma cases. Cytoplasmic Shh staining significantly correlated with a lower tumor grade. Next, the in vitro effects of two Hh signaling pathway inhibitors on breast cancer cell lines were evaluated using the Smoothened (SMO) antagonist GDC-0449 and the direct GLI1 inhibitor GANT-61. GDC-0449 and GANT-61 exhibited the following effects: a) inhibited breast cancer cell survival; b) induced apoptosis; c) inhibited Hh pathway activity by decreasing the mRNA expression levels of GLI1 and Ptch and inhibiting the nuclear translocation of GLI1; d) increased/decreased EGFR and ErbB2 protein expression, reduced p21-Ras and ERK1/ERK2 MAPK activities and inhibited AKT activation; and e) decreased the nuclear translocation of NF-κB.
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CAS 500579-04-4 GANT-61

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