GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.
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.