Catalog No.: PC-24681Not For Human Use, Lab Use Only.
HIF-1α inhibitor LW6 is a specific small compound that inhibits the accumulation of HIF-1α, decreases HIF-1α protein expression without affecting HIF-1β expression, has IC50 of 2.6 uM in HIF-1-mediated cell-based reporter assay in Hep3B cells.
HIF-1α inhibitor LW6 is a specific small compound that inhibits the accumulation of HIF-1α, decreases HIF-1α protein expression without affecting HIF-1β expression, has IC50 of 2.6 uM in HIF-1-mediated cell-based reporter assay in Hep3B cells. LW6 promoted the degradation of wild type HIF-1α, but not of a DM-HIF-1α with modifications of P402A and P564A, at hydroxylation sites in the oxygen-dependent degradation domain (ODDD). LW6 does not affect the activity of prolyl hydroxylase (PHD), but induced the expression of von Hippel-Lindau (VHL), which interacts with prolyl-hydroxylated HIF-1α for proteasomal degradation. LW6 demonstrated strong anti-tumor efficacy in vivo and caused a decrease in HIF-1α expression in frozen-tissue immunohistochemical staining in mice carrying xenografts of human colon cancer HCT116 cells.
