500579-04-4

Inhibitor of Hedgehog (Hh) signalling pathway. Blocks the GLI function which constitutes the final step in the Hh pathway. Interferes with GLI1 DNA binding in living cells. Inhibits cell proliferation of tumor cells in vitro in a GLI-dependent manner. Blocks cell growth in an in vivo xenograft model using human prostate cancer cells.

ChEBI: GANT61 is an aminal that is hexahydropyrimidine which is substituted on each nitrogen by a 2-(dimethylamino)benzyl group, and at the aminal carbon by a pyridin-4-yl group. A Hedgehog signaling pathway and Gli protein inhibitor. It has a role as a Hedgehog signaling pathway inhibitor, a glioma-associated oncogene inhibitor, an antineoplastic agent and an apoptosis inducer. It is a tertiary amino compound, a member of pyridines, a substituted aniline and an aminal.

GANT61 blocks hedgehog pathway signaling by inhibiting the transcripional activity of Gli1 (IC50 = 5 μM). GANT 61 led to a regression of 22Rv1 human prostate tumor cell xenografts in nude mice.

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