Hypoxia inducible factors (HIFs) are heterodimeric proteins belonging to the basic helix-loop-helix-PAS (bHLH/PAS) family of transcription factors that mediate the primary transcriptional response to stress caused by hypoxia (accessible O2 level < 2%). HIFs are characterized by containing two subunits, including O2-labile α subunit (HIFα) and constitutively expressed β subnit (HIFβ). Mammalian HIFα consists of three isoforms, including HIF1α, HIF2α and HIF3α, which play an essential role in the regulation of HIF activity by O2 availability. Under normal O2 tension, HIFα is hydroxylated at the two conserved proline residues within the O2-dependent degradation (ODD) domain by prolylhydroxylase domain proteins (PHDs) and undergoes proteosomal degradation catalyzed by a complex formed by E3 ubiquitin ligase and the von Hippel-Lindau protein (pVHL); while, under hypoxia, HIFα stabilizes with PHDs being deactivated and hence induce transcription of genes with adaptive functions.
- Cat.No. Product Name Information
- B1115 BAY 87-2243 BAY 87-2243 is a selective inhibitor of HIF-1 induced gene activation .
- A4509 PX 12 Competitive, irreversible thioredoxin-1 (Trx-1) inhibitor (Ki = 31 μM) that attenuates expression of HIF-1α, VEGF and iNOS (IC50 values are 7.2, ~10 and 18.1 μM respectively). Exhibits antitumor activity; directly inhibits tubulin polymerization in vitro and decreases tumor microvessel density in vivo.
- A4508 ML 228 HIF pathway activator (EC50 values are 1.23 and 1.4 μM for HRE gene reporter assay and HIF-1α nuclear translocation assay respectively); acts via chelation of iron, independently of PHD. Also exhibits > 80% inhibition of the human A3 receptor, dopamine transporter, μ receptor, hERG and 5-HT2B receptor, and rat sodium channel site 2, at a concentration of 10 μM.
- A4507 KC7F2 Inhibitor of HIF-1α. Thought to act via down-regulation of HIF-1α protein synthesis; reduces phosphorylation of eIF4E binding protein 1 (4EBP1) and p70 S6K in hypoxic conditions. Also blocks hypoxia-induced HIF-1α accumulation in a range of human cancer cell lines. Inhibits the expression of HIF target genes, such as carbonic anhydrase IX and MMP2.
- A4505 Chetomin Chetomin, an antibiotic metabolite of chaetomium cochliodes, is an inhibitor of HIF-1 by weaken transcription of HIF-1 and recently is raised interests as a cancer chemotherapeutic agent.
IOX2(Glycine) is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.
- A4188 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2), an endogenous metabolite of 17β-estradiol (E2), is an inhibitor of microtubule assembly that inhibits the polymerization of tubulin and interferes with mitotic spindle dynamics leading to the blockage of mitosis of human cancer cells which lack estrogen receptors in metaphase.
FG-4592 (also known as ASP1517), 2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic acid, is a potent small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH), an enzyme up-regulating the expression of endogenous human erythropoietin (Epo).
- C4672 IOX4
- B6004 PX-478 2HCl
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