M1001 is the first HIF-2 allosteric agonist, capable of altering the conformation of Tyr281 of the HIF-2α PAS-B domain and enhancing the affinity of HIF-2α and ARNT for transcriptional activation.

TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 disrupts HIF-2α-ARNT heterodimerization by binding to HIF-2α PAS-B domain, decreases DNA-binding activity, and reduces HIF-2α target gene expression.

PHD-1 inhibitor C17 is an early lead compound of 4-{[1,2,4]triazolo[1,5-a]pyridin-5-yl}benzonitrile-based inhibitors of the hypoxia-inducible factor (HIF) prolylhydroxylase domain-1 (PHD-1) showing a moderate rate of microsomal turnover in vitro.

PT2385 is an inhibitor of hypoxia inducible factor (HIF)-2 alpha with antineoplastic effect.

JNJ-42041935 is a selective inhibitor of prolyl hydroxylase (PHD) with the pKis of 7.91 ± 0.04, 7.29 ± 0.05, and 7.65 ± 0.09 for PHD1, PHD2, and PHD3, respectively.

Enarodustat is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM; Enarodustat has entered clinical trial for renal anemia.

IDF-11774 is a hypoxia-inducible factor (HIF)-1α inhibitor which regulates cancer metabolism, thereby suppressing tumor growth.

HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay.

SYP-5 is a HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.

Oltipraz can inhibit the insulin-activated HIF-1α (IC50 = 10 µM) in a time-dependent manner.

VHL032-C6-carboxylic acid is a PROTAC block consist of VHL032 linked to alkyl with a carboxylic acid functional group for conjugation reactions.