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Home > Inhibitors & Agonists > Nuclear Receptor/Transcription Factor > HIF/HIF Prolyl-hydroxylase

HIF/HIF Prolyl-hydroxylase

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Cat. No. Product Name Field of Application Chemical Structure
DC41030 1,4-DPCA ethyl ester Featured
1,4-DPCA ethyl ester is the ethyl ester of 1,4-DPCA and can inhibit factor inhibiting HIF (FIH).
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DC47980 HIF-2α-IN-4 Featured
HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing.
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DC73836 MO-2097
MO-2097 is a small molecule hnRNPA2B1-binding compound (ITC KD=43.1 uM) that suppresses hnRNPA2B1-induced HIF-1α protein expression under hypoxic and mimetic hypoxia.
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DC73835 FG-0041
FG-0041 (FG0041) is a small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 of 2 uM for collagen prolyl hydroxylase.
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DC73834 ER-400583-00
ER-400583-00 is a small-molecule HIF-1α inhibitor, inhibits the induction of HIF-1 reporter activity in response to hypoxia with IC50 of 7.9 nM.
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DC7486 PX-478 2HCL Featured
PX-478 is an inhibitor of HIF-1a with an IC50 of 20-30μM enhances radiosensitivity of prostate carcinoma cells.
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DC72867 Belzutifan
Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay). PT2977 demonstrated high potency with EC50 of 17 nM in the VEGFA secretion assay in 786-O cells. PT2977 (0.3, 1, and 3 mg/kg, oral) potently and dose-dependently reduced mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, exhibited excellent antitumor activity in the 786-O mouse xenograft model In phase 1 clinical, PT2977 decreased in the HIF-2α target erythropoietin (EPO) following once daily oral administration of PT2977 at the dose levels of 20, 40, 80, 120, 160, and 240 mg in patients with solid tumors, also showed encouraging outcomes in patients with advanced renal cell carcinoma in an expansion cohort of 55 patients with ccRCC treated at 120 mg q.d.
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DC10464 PT2385 Featured
PT2385 is an orally active, small molecule inhibitor of hypoxia inducible factor (HIF)-2alpha, with potential antineoplastic activity.
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DC8390 Oltipraz Featured
Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.
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DC8447 KC7F2 Featured
KC7F2 is a potent HIF-1 pathway inhibitor and that its potential as a cancer therapy agent warrants further study.
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DC8166 Molidustat(BAY 85-3934) Featured
Hypoxia-inducible factor prolyl hydroxylase inhibitor
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DC5193 Roxadustat(FG-4592) Featured
FG-4592 is an HIF αprolyl hydroxylase inhibitor, stabilizes HIF-2 and induces EPO production.
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DC8188 Daprodustat Featured
Daprodustat(GSK1278863) isa HIF-prolyl hydroxylase inhibitor.
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DC9044 2-Methoxyestradiol Featured
2-methoxyestradiol (2ME2; NSC-659853) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 ± 0.11 μM for the inhibition of BPAEC migration.
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DC72414 Steppogenin
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors.
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DC71830 Zifcasiran
Zifcasiran is a hypoxia-inducible factor (HIF) synthesis reducer. Zifcasiran shows antitumor activities and can be used in advanced renal cell carcinoma research.
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DC71829 Mersalyl
Mersalyl (Salirgan) is a potent vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1) inducer. Mersalyl induces VEGF and ENO1 mRNA expression. Mersalyl shows diuresis effects.
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DC71180 GEM-5
GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.
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DC71012 BNS
BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor.
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DC10339 Vadadustat Featured
Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.
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DC70919 YQ-0629
YQ-0629 is a specific HIF-2α inhibitor, binds to HIF-2α PAS-B domain with Kd of 57.5 uM.YQ-0629 could inhibit the expression of HIF-2α with or without the presence of PTX (3 nM) in MCF7 MS culture, does not bind to HIF-1α or affect the expression of HIF-1α.YQ-0629 suppresses self-renewal capacity and synergizes with PTX to reverse the chemoresistance of MCF7 MS.YQ-0629 inhibits growth of BCSCs derived from breast cancer patients and synergistically increases anti-BCSCs activity of PTX in vivo.
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DC70551 KUSC-5037
KUSC-5037 (KUSC5037) is a novel effective HIF-1 inhibitor with IC50 of 1.2 uM against HIF-1 transcriptional activity.KUSC-5037 suppressed the HIF-1α (a regulatory subunit of HIF-1) mRNA, causing decreases in the gene expression of HIF-1 target genes such as carbonic anhydrase 9 (CA9) and vascular endothelial growth factor (VEGF) genes.KUSC-5037 directly targets ATP5B protein, a catalytic β subunit of mitochondrial FoF1-ATP synthase.
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DC70485 HIF inhibitor 208
HIF inhibitor 208 is a small molecule inhibitor of HIF pathway with IC50 of 0.5 nM.
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DC49824 HIF-1α-IN-2
HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation.
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DC49823 HIF-PHD-IN-2
HIF-PHD-IN-2 (compound 25) is a potent PHD inhibitor with IC50s of <100 nM for PHD1, PHD2 and PHD3, respectively.
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DC49822 HIF-2α-IN-5
HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of < 50 nM.
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DC49821 KUSC-5001
KUSC-5001 is a potent HIF-1 inhibitor with an IC50 of 18 μM. Hypoxia-inducible factor 1 (HIF-1) plays a pivotal role in tumor survival and malignancy.
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DC11607 JTZ-951(Enarodustat) Featured
A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.
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DC9811 PT2399 Featured
PT2399(PT=2399) is a novel HIF2α Antagonist.
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DC11782 IDF-11774 Featured
IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.
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