1,4-DPCA ethyl ester is the ethyl ester of 1,4-DPCA and can inhibit factor inhibiting HIF (FIH).

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.

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.

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.

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.

PX-478 is an inhibitor of HIF-1a with an IC50 of 20-30μM enhances radiosensitivity of prostate carcinoma cells.

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.

PT2385 is an orally active, small molecule inhibitor of hypoxia inducible factor (HIF)-2alpha, with potential antineoplastic activity.

Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.

KC7F2 is a potent HIF-1 pathway inhibitor and that its potential as a cancer therapy agent warrants further study.

Hypoxia-inducible factor prolyl hydroxylase inhibitor

FG-4592 is an HIF αprolyl hydroxylase inhibitor, stabilizes HIF-2 and induces EPO production.

Daprodustat(GSK1278863) isa HIF-prolyl hydroxylase inhibitor.

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.

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.

Zifcasiran is a hypoxia-inducible factor (HIF) synthesis reducer. Zifcasiran shows antitumor activities and can be used in advanced renal cell carcinoma research.

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.

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.

BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor.

Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.

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.

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.

HIF inhibitor 208 is a small molecule inhibitor of HIF pathway with IC50 of 0.5 nM.

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.

HIF-PHD-IN-2 (compound 25) is a potent PHD inhibitor with IC50s of <100 nM for PHD1, PHD2 and PHD3, respectively.

HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of < 50 nM.

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.

A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.

PT2399(PT=2399) is a novel HIF2α Antagonist.

IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.