cyclo(CLLFVY)

Description: Cyclo(CLLFVY) is an inhibitor of hypoxia-inducible factor-1 (HIF-1), exhibiting half-maximal inhibitory concentrations (IC50) of 19 µM in U2OS cells and 16 µM in MCF-7 cells. It binds to the PAS-B domain of HIF-1alpha, inhibiting the dimerization and transcriptional activity of HIF-1. Moreover, cyclo(CLLFVY) downregulates the expression of hypoxia response genes (such as VEGF and CAIX), demonstrating antitumor effects against HIF-1-related cancers. Target: VEGFR, HIF/HIF Prolyl-Hydroxylase. Smiles: C([C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)[C@H](C(C)C)NC1=O)C3=CC=CC=C3