Description: GANT 58 (NSC-75503) is a potent antagonist of Gli. Which inhibits GLI1-induced transcription (IC50: 5 µM). Target: Hedgehog/Smoothened. Smiles: c1cc(ccn1)-c1sc(c(c1-c1ccncc1)-c1ccncc1)-c1ccncc1. References: Lauth M, et al. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule...

Hedgehog (hh) proteins, important regulators of development, bind the cell-surface protein Patched, allowing activation of Smoothened (Smo). 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...