Cyclo(CLLFVY) is a selective inhibitor of hypoxia-inducible factor-1 (HIF-1), demonstrating IC50 values of 19 μM in U2OS cells and 16 μM in MCF-7 cells. By binding to the PAS-B domain of HIF-1α, cyclo(CLLFVY) effectively disrupts HIF-1 dimerization and subsequent transcriptional activity. This compound downregulates the expression of key hypoxia response genes, including VEGF and CAIX, and shows potential for antitumor applications in HIF-1 associated cancers.
Cyclo(CLLFVY) is a selective inhibitor of hypoxia-inducible factor-1 (HIF-1), demonstrating IC50 values of 19 μM in U2OS cells and 16 μM in MCF-7 cells. By binding to the PAS-B domain of HIF-1α, cyclo(CLLFVY) effectively disrupts HIF-1 dimerization and subsequent transcriptional activity. This compound downregulates the expression of key hypoxia response genes, including VEGF and CAIX, and shows potential for antitumor applications in HIF-1 associated cancers.
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