GANT 61

Name: GANT 61
Brand: Tocris Bioscience
SKU: 3191

Tocris Bioscience a Bio-Techne Brand

Catalog # 3191

Citations (5)

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Key Product Details

Description:	GLI antagonist; inhibits Hedgehog (Hh) signaling
Chemical Name:	2,2'-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine
Purity:	≥98% (HPLC)
Molecular Weight:	429.61

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Biological Activity for GANT 61

GANT 61 is a GLI antagonist that inhibits GLI1 and GLI2-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. Inhibits the pluripotency factors Oct4, Sox-2, Nanog and c-Myc in pancreatic cancer stem cells.

Compound Libraries for GANT 61

GANT 61 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for GANT 61

M. Wt	429.61
Formula	C₂₇H₃₅N₅
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	500579-04-4
PubChem ID	421610
InChi Key	KVQOGDQTWWCZFX-UHFFFAOYSA-N
Smiles	CN(C1=CC=CC=C1CN2CCCN(CC4=C(N(C)C)C=CC=C4)C2C3=CC=NC=C3)C

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 for GANT 61

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	21.48	50
	ethanol	42.96	100

Preparing Stock Solutions for GANT 61

The following data is based on the product molecular weight 429.61.

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
1 mM	2.33 mL	11.64 mL	23.28 mL
5 mM	0.47 mL	2.33 mL	4.66 mL
10 mM	0.23 mL	1.16 mL	2.33 mL
50 mM	0.05 mL	0.23 mL	0.47 mL

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References for GANT 61

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

Fu GANT-61 inhibits pancreatic cancer stem cell growth in vitro and in NOD/SCID/IL2R gamma null mice xenograft. Cancer Lett. 2012 PMID: 23200667
Mazumdar Blocking Hedgehog survival signaling at the level of the GLI genes induces DNA damage and extensive cell death in human colon carcinoma cells. Cancer Res. 2011 PMID: 21747117
Lauth Inhibition of GLI-mediated transcription and tumor cell growth by small molecule antagonists. Proc.Natl.Acad.Sci.USA 2007 PMID: 17494766

Citations for GANT 61 (5)

Showing 1 - 5 of 5 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for GANT 61 include:

Calcaterra et al. (2018) Chemical, computational and functional insights into the chemical stability of the Hedgehog pathway inhibitor GANT61. J Enzyme Inhib Med Chem. 33:349
PMID: 29338454
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
Lim et al. (2015) Mitochondria-derived reactive oxygen species drive GANT61-induced mesothelioma cell apoptosis. Oncotarget. 6:1519
PMID: 25544756
Todd and Fischer (2015) Hedgehog signaling stimulates the formation of proliferating Müller glia-derived progenitor cells in the chick retina. Development. 142:2610
PMID: 26116667
Wellbrock et al. (2015) Expression of Hedgehog Pathway Mediator GLI Represents a Negative Prognostic Marker in Human Acute Myeloid Leukemia and Its Inhibition Exerts Antileukemic Effects. Clin Cancer Res. 21:2388
PMID: 25745035

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