Stemcell, 73692, GANT61

GANT61 is a hexahydropyrimidine derivative which selectively inhibits GLI transcription factors in the Hedgehog signaling pathway. GANT61 acts downstream of Smoothened to inhibit both GLI1- and GLI2-mediated transcription (IC₅₀ = 5 μM in a GLI-transfected cell line) by preventing their DNA binding (Lauth et al.).

CANCER RESEARCH

· Inhibits in vitro proliferation of cancer cell lines (PANC1 and 22Rv1) with elevated GLI1 levels, and prevents the development of 22Rv1 tumors in mice (Lauth et al.).

· Inhibits pancreatic cancer stem cell growth in vitro and in mouse xenograft model (Fu et al.)

· Induces cell death of primitive neuroectodermal tumor cell line in a caspase-independent manner by inhibiting DNA replication (Matsumoto et al.).

· Causes apoptosis in myeloid leukemia cells and in some cell lines is more effective when combined with rapamycin (Pan et al.).