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HIF Hypoxia-inducible factors

Inhibitors

Cat.No.  Name Information
M1992 2-Methoxyestradiol 2-methoxyestradiol (2-ME2), an endogenous metabolite of 17β -estradiol (E2) with oral activity, is an apoptosis inducer and angiogenesis inhibitor with effective antitumor activity. Methoxyestradiol can also destabilize microtubules. Methoxyestradiol is a potent inhibitor of superoxide dismutase (SOD) and reactive oxygen species (ROS) that can induce autophagy in transformed cell line HEK293, cancer cell line U87 and HeLa.
M9066 PT2385 PT2385 is an orally active, selective inhibitor of hypoxia inducible factor (HIF)-2alpha, with a Ki value of less than 50 nM.
M2558 DMOG DMOG (Dimethyloxaloylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolyl hydroxylase.
M21408 Verucopeptin Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor that reduces the expression of HIF-1 target genes and the protein level of HIF-1α. It is commonly used for cancer-related studies.
M20749 TP0463518 TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. TP0463518 inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively.
M14450 IDF-11774 IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.
M14449 HIF-2α-IN-1 HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay.
M14448 Echinomycin Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.
M14447 Acriflavine hydrochloride Acriflavine hydrochloride (Acriflavinium chloride hydrochloride) is a fluorescent acridine dye that can be used to label nucleic acid.
M14446 Acriflavine Acriflavine is a fluorescent dye for labeling high molecular weight RNA. It is also a topical antiseptic.
M11025 M1001 M1001 is a weaker HIF-2α agonist that binds directly to the HIF-2α PAS-B domain.Kd The value is 667 nM. The M1001 enhances stability between HIF-2α-ARNT complexes.
M11006 IOX4 IOX4 is a selective PHD2 inhibitor,IC50 With a value of 1.6 nM, HIFα expression is induced in cells and wild-type mice to permeate the blood-brain barrier. IOX4 competes with and displaces 2-oxoglutaric acid (2OG) at the PHD2 active site.
M10501 PT2399 PT2399 is a potent and orally available antagonist of HIF-2 with an IC50 of 6 nM, PT2399 selectively disrupts the heterodimerization of HIF-2α with HIF-1β.
M10436 Belzutifan (PT2977) Belzutifan (PT2977) is a second-generation orally active and selective HIF-2α inhibitor with an IC50 of 9 nM.
M10169 Vadadustat Vadadustat is a novel, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor.
M9842 ML228 ML228 is a potent the HIF pathway activator, with EC50 values of 1.23 and 1.4 μM for HRE gene reporter assay and HIF-1α nuclear translocation assay respectively.
M9675 Desidustat Desidustat is an inhibitor of HIF hydroxylase.
M9279 LW6 LW6 is a novel HIF-1alpha inhibitor, with an IC50 of 4.4 μM.
M9198 JTZ-951 Enarodustat (JTZ-951) is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM.
M9066 PT2385 PT2385 is an orally active, selective inhibitor of hypoxia inducible factor (HIF)-2alpha, with a Ki value of less than 50 nM.
M8963 JNJ-42041935 JNJ-42041935 is a potent, competitive, reversible, and selective inhibitor of PHD with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09 for PHD1, PHD2, and PHD3, respectively.
M8924 Daprodustat Daprodustat (GSK1278863) is a novel, orally active inhibitor of hypoxia-induced factor prolyl hydroxylase (HIF-PHI). Reversible inhibition of HIF-PHD activity under normal partial oxygen pressure can temporarily inhibit HIF-α degradation and promote the expression of related hypoxia metabolism genes.
M8678 FG-2216 (BIQ) BIQ (FG-2216) is an orally available and potent inhibitor of prolyl-hydroxylase (PHD) with IC50 of 3.9 uM for PDH2 enzyme.



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