HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under poxia. HIF-1α-IN-5 can be used in the research of cancer.
HIF-1α-IN-5 (compound 15, 24 h) shows inhibitory effects against HIF-1α transcription in HEK293T cells, with an IC50 value of 24 nM[1].HIF-1α-IN-5 (0-50 μM, 24 h) downregulates VEGF and PDK1 mRNA expressions under poxia in HEK293T cells[1].HIF-1α-IN-5 (10 μM) inhibits MAO-A activity activity by 80.64%, and ADORA2A by 43.95%[1].
References:
[1]. Zian Xue, et al. Benzo[d]isoxazole Derivatives as poxia-Inducible Factor (HIF)-1α Inhibitors. ACS Med. Chem. Lett. 2022.