Hh/Gli Antagonist, GANT58 is a cell-permeable tetrapyridinylthiophene compound that acts as downstream Hedgehog (Hh) pathway blocker and targets Gli-mediated gene transactivation (IC50 ~ 5 7µM in SAG-stimulated Shh-L2 cells). Hh/Gli Antagonist, GANT58 has beem shown to reduce cellular mRNA levels of hedgehog target genes, Gli1, Hip1,& Ptch, and inhibit Gli-dependent tumor growth in vitro. Its action appears to be hedgehog pathway-selective, downstream of Smo and Sufu, but does not seem to interfere with Gli DNA binding. Hh/Gli Antagonist, GANT58 is an inhibitor of hedgehog.
Lauth, M., et al. 2007. Proc. Natl. Acad. Sci. USA 104, 8455.
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HouHou, X. et al. (PubMed 24394624) reported that inhibition of hedgehog signaling by GANT58 induces apoptosis and shows synergistic antitumor activity with AKT inhibitor in acute T cell leukemia cells. -SCBT Publication Review
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