GANT61, 10 mg

From STEMCELL Technologies, GANT61 is a hexahydropyrimidine derivative that selectively inhibits GLI transcription factors in the Hedgehog signaling pathway. It acts downstream of Smoothened to inhibit both GLI1- and GLI2-mediated transcription (IC50 = 5 µM in a GLI-transfected cell line) by preventing their binding to DNA. The compound is supplied as a crystalline solid with a purity of ≥ 98% and a molecular weight of 429.6 g/mol. It is stable for 12 months from date of receipt when stored at -20°C and protected from prolonged exposure to light; long-term storage should include a desiccant. The compound has low solubility in aqueous media, with a solubility of ≤ 2.3 mM in absolute ethanol. Stock solutions should be prepared fresh before use, and final ethanol concentration in cell culture should be kept below 0.1% to avoid potential cell toxicity. Published applications include inhibition of in vitro proliferation of cancer cell lines with elevated GLI1 levels, suppression of pancreatic cancer stem cell growth in vitro and in mouse xenograft models, induction of cell death in a primitive neuroectodermal tumor cell line in a caspase-independent manner, and apoptosis in myeloid leukemia cells, with enhanced effectiveness in some lines when combined with Rapamycin.