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.
HIF inhibitors/modulators
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S1007 | Roxadustat (FG-4592) | Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilises HIF-2 and induces EPO production. This compound also potentiates RSL3 induced ferroptosis. Phase 3. |
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| 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). |
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| S8351 | PT2399 | PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β. |
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| 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 stabilises HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycaemic 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. |
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| S1233 | 2-Methoxyestradiol (2-MeOE2) | 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerises microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. This compound also induces both autophagy and apoptosis in various carcinogenic cell lines. |
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| S7612 | PX-478 Dihydrochloride | PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1 alpha (HIF-1 alpha) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1. |
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| 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. |
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| S7946 | KC7F2 | KC7F2 is a selective HIF-1α translation inhibitor with an IC50 of 20 μM in a cell-based assay. |
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| S7958 | Lificiguat (YC-1) | Lificiguat (YC-1) is a nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha). |
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| 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. |
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