Chemical Name: 2,2'-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine
Biological ActivityGANT 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.
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Blocking Hedgehog survival signaling at the level of the GLI genes induces DNA damage and extensive cell death in human colon carcinoma cells.
Mazumdar T, Devecchio J, Agyeman A et al.
GANT-61 inhibits pancreatic cancer stem cell growth in vitro and in NOD/SCID/IL2R gamma null mice xenograft.
Fu et al.
Cancer Lett., 2012;330:22
Inhibition of GLI-mediated transcription and tumor cell growth by small molecule antagonists.
Lauth et al.
Citations for GANT 61
The citations listed below are publications that use Tocris products. Selected citations for GANT 61 include:
5 Citations: Showing 1 - 5
Chemical, computational and functional insights into the chemical stability of the Hedgehog pathway inhibitor GANT61.
Authors: Calcaterra Et al.
J Enzyme Inhib Med Chem 2018;33:349
Pharmacological targeting of GLI1 inhibits proliferation, tumor emboli formation and in vivo tumor growth of inflammatory breast cancer cells.
Cancer Lett 2017;411:136
Mitochondria-derived reactive oxygen species drive GANT61-induced mesothelioma cell apoptosis.
Authors: Lim Et al.
Expression of Hedgehog Pathway Mediator GLI Represents a Negative Prognostic Marker in Human Acute Myeloid Leukemia and Its Inhibition Exerts Antileukemic Effects.
Authors: Wellbrock Et al.
Clin Cancer Res 2015;21:2388
Hedgehog signaling stimulates the formation of proliferating Müller glia-derived progenitor cells in the chick retina.
Authors: Todd and Fischer
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