HIF-1α-IN-2

HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase

IC50: 28 nM (HIF-1α) in MDA-MB-231, 15 nM (HIF-1α) in MiaPaCa-2[1]

HIF-1α-IN-2 (compound 7f) (5 μM; 72h) suppresses the viability of MDA-MB-231 and MiaPaCa-2 cells with IC50s of 28 nM and 15 nM, respectively[1]. HIF-1α-IN-2 (0-1 μM; 72h) suppresses the expression of HIF-1α and VEGF with dose-dependent effect[1]. HIF-1α-IN-2 (0.25, 0.5, and 1 µM; 16-24h) can significantly inhibit the migration of MDA-MD-231 cells by 56% (0.25 µM), 83% (0.5 µM), and 85% (1 µM), respectively, and also noted in MiaPaCa-2 cells, which demonstrates the unique anti-migration effect of HIF-1α-IN-2[1]. HIF-1α-IN-2 (0-1 μM; 72h) suppresses HIF-1α mRNA levels in MDA-MB-231 cells under hypoxia[1]. Cell Viability Assay Cell Line: MDA-MB-231 cells, MiaPaCa-2 cells[1] Concentration: 5 μM Incubation Time: 72 hours Result: Suppressed the viability of these two cell lines with IC50 of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively. Cell Viability Assay Cell Line: MDA-MB-231 cells, MiaPaCa-2 cells[1] Concentration: 5 μM Incubation Time: 72 hours Result: Suppressed the viability of these two cell lines with IC50 of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively.

[1]. Wu YC, et al. Synthesis and evaluation of biarylquinoline derivatives as novel HIF-1α inhibitors. Bioorg Chem. 2022;121:105681.