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HIF Inhibitors | Activators (7)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
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. Phase 3.
S1233 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2.
  • Nucleic Acids Res, 2015, 10.1093/nar/gkv379
  • Oncotarget, 2015, 6(4):2250-62
  • Nitric Oxide, 2015, 46:192-203
S2919 IOX2 IOX2 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.
  • Arch Toxicol, 2015, 10.1007/s00204-015-1549-y
  • Nitric Oxide, 2015, 46:192-203
  • Int J Low Extrem Wounds, 2015, 14(1):63-72
S7309 BAY 87-2243 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.
  • Vascul Pharmacol, , 10.1016/j.vph.2016.05.002
S7612 PX-478 2HCl PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.
  • Biochem Biophys Res Commun, 2015, 463(1-2):130-6
S7979 FG-2216 FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2.
S7946 KC7F2 KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1007 Roxadustat (FG-4592) <1 mg/mL 70 mg/mL <1 mg/mL
S1233 2-Methoxyestradiol (2-MeOE2) <1 mg/mL 60 mg/mL <1 mg/mL
S2919 IOX2 <1 mg/mL 7 mg/mL <1 mg/mL
S7309 BAY 87-2243 <1 mg/mL <1 mg/mL 8 mg/mL
S7612 PX-478 2HCl 78 mg/mL 78 mg/mL 78 mg/mL
S7979 FG-2216 <1 mg/mL 56 mg/mL <1 mg/mL
S7946 KC7F2 <1 mg/mL 100 mg/mL <1 mg/mL
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