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.
GANT-61 (40 mg/kg, i.p., three days per week) inhibits CSC tumor growth in NOD/SCID IL2Rγ null mice[2]. GANT61 (50 mg/kg, p.o.) enhances the effects of chemotherapeutic drugs used in the treatment of neuroblastoma in an additive or synergistic manner and reduces the growth of established neuroblastoma xenografts in nude mice[3].
![2,2'-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine Structure](/CAS/GIF/500579-04-4.gif)
![2,2'-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine pictures](https://img.chemicalbook.com/ProductImageEN/2019-12/Small/10552f29-11d0-4cba-bcfe-100e1b47e480.jpg)