Hedgehog proteins, important regulators of development, bind the cell-surface protein Patched, allowing activation of Smoothened. In vertebrates, this ultimately leads to the activation of the zinc-finger transcription factors of the GLI family. Overactivation of this pathway contributes to certain cancers, including glioblastoma, for which the GLI proteins are named. GANT 61 is a GLI antagonist, inhibiting GLI1 activation of gene expression with an IC50 value of 5 μM. It does not affect signaling through NF-κB, glucocorticoid receptor, MAPK, HGF, C/EBPα, or HIF-1, supporting specificity for the Hedgehog pathway. GANT 61 has been shown to inhibit the in vitro proliferation of PANC-1 and 22Rv1 cancer cells, which have elevated GLI1 levels, and prevent the development of 22Rv1 tumors in mice.
![2,2'-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine](https://www.chemicalbook.com/CAS/GIF/500579-04-4.gif)
