Home Angiogenesis HIF

HIF Inhibitors/Modulators

Hypoxia-inducible factor (HIF) activates the transcription of genes that are involved in crucial aspects of cancer biology, including angiogenesis, cell survival, glucose metabolism and invasion.HIF-1α protein synthesis is regulated by activation of the phosphatidylinositol 3-kinase (PI3K) and ERK mitogen-activated protein kinase (MAPK) pathways. Then AKT, mTOR and p70 S6 kinase (S6K) are phosphorylated resulting in the inhibition of cap-dependent mRNA translation through binding of 4E-BP1 to eIF-4E. The effect of growth-factor signalling is an increase in the rate at which a subset of mRNAs within the cell (including HIF-1α mRNA) is translated into protein.

Other Angiogenesis Related Inhibitors

Src FGFR Bcr-Abl Syk VDA FLT3 FAK BTK ANGPTL FLT

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S1007 Roxadustat (FG-4592) Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. This compound also potentiates RSL3 induced ferroptosis. Phase 3.
Immunity, 2025, S1074-7613(25)00139-6
Cell Stem Cell, 2025, S1934-5909(25)00338-8
Mol Cell, 2025, 85(15):2973-2987.e6
Verified customer review of Roxadustat (FG-4592)
S8886 PT2977 (Belzutifan) Belzutifan (PT2977), an orally active and selective HIF-2α inhibitor, increases potency and improves pharmacokinetic profile, providing a potential treatment for clear cell renal cell carcinoma (ccRCC).
Cell Death & Differentiation, February 26, 2025, 1473-1483
Cell Death Discovery, August 14, 2025, 380
Cell Death Differ, 2025, 10.1038/s41418-025-01469-9
S8351 PT2399 PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.
Nat Commun, 2025, 16(1):4681
Cell Stress, 2024, 8:1-20
S5742 Deferoxamine mesylate Deferoxamine mesylate is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy.Please do not prepare stock solutions with normal saline or PBS, as precipitation may occur.
Cancer Cell, 2025, S1535-6108(25)00132-1
Nat Commun, 2025, 16(1):4919
Nat Commun, 2025, 16(1):6617
S7925 Deferoxamine Deferoxamine (Deferoxamine B, Deferrioxamine) is an iron chelator and a reversible inhibitor of S-phase in DNA synthesis. It enhnaces HIF-1α activation by inhibiting prolyl hydroxylase activity, activating insulin receptor (InsR) and Glut1. It also increases phosphorylation of Akt/PKB, FoxO1, GSK3β, influencing gluconeogenesis and glycogen synthesis, while reducing oxidative stress in diabetic hyperglycemia. It can be used to reduce iron accumulation and deposition in tissues and in studies of neurodegenerative diseases, anti-cancer and anti-COVID-19.
Redox Biol, 2025, 86:103865
J Nanobiotechnology, 2025, 23(1):703
Mater Today Bio, 2025, 34:102206
S1233 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. This compound also induces both autophagy and apoptosis in various carcinogenic cell lines.
Nat Commun, 2025, 16(1):4681
Int J Nanomedicine, 2025, 20:933-950
Theranostics, 2024, 14(13):5123-5140
Verified customer review of 2-Methoxyestradiol (2-MeOE2)
S7612 PX-478 Dihydrochloride PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.
PLoS Pathogens, September 18, 2017, e1006628
Frontiers in Oncology, May 8, 2025, 1564655
Gut, February 9, 2026, gutjnl-2025-336161
Verified customer review of PX-478 Dihydrochloride
S7309 BAY 87-2243 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. This compound inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. It exerts antitumor activity. Phase 1.
Cancer Sci, 2025, 116(8):2113-2124
Cancer Sci, 2025, 10.1111/cas.70102
Hum Reprod Open, 2024, 2024(1):hoae002
Verified customer review of BAY 87-2243
S7946 KC7F2 KC7F2 is a selective HIF-1α translation inhibitor with IC50 of 20 μM in a cell-based assay.
International Journal of Oncology, October 6, 2025, 100
Investigative Ophthalmology & Visual Science, June 1, 2022, 13
bioRxiv, July 1, 2025, nan
Verified customer review of KC7F2
S2919 IOX2 IOX2 (JICL38) is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.
Cell Rep Med, 2024, 5(2):101400
Int J Mol Sci, 2024, 26(1)117
Oncogene, 2022, 41(13):1944-1958
Verified customer review of IOX2

Signaling Pathway Map