hif-phd2

Adaptaquin is an inhibitor of the hypoxia-inducing factor prolyl hydroxylase (HIF-PH) [1] [2].

HIF-PHD-IN-1 is a pharmacological compound that acts as an orally active inhibitor of the hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), displaying an IC50 of 54 nM for hHIF-PHD2. Its potential as a therapeutic agent for renal anemia is highly promising.

IOX2 (IOX 2) is a selective inhibitor of the Hypoxia Inducible Factor (HIF) Prolyl-Hydroxylases (PHD); active in cells with the IC50 value of 21 nM for PHD2/ELGN-1 and no inhibition at FIH (20uM).

KRH102140 is a PHD2 activator that reduces angiogenesis by inhibiting HIF-1alpha, used in cardiovascular disease research.

ZG-2305 is a selective, orally active inhibitor of FIH with Ki values of 79.6 nM and 2786 nM for FIH and PHD2, respectively. It increases EGLN3 gene expression, reduces cellular triglyceride levels, and decreases lipid accumulation, making it suitable for obesity and fatty liver disease research.

HIF-PHD-IN-4 (Compound 13) is an orally active PHD2 inhibitor with an IC50 of 100 nM. At a dose of 2 mg/kg, it effectively enhances G-CSF-induced mobilization of hematopoietic stem cells in mice. HIF-PHD-IN-4 is suitable for research in the oncology field.

IOX5 is a selective prolyl hydroxylase (PHD) inhibitor with an IC50 of 0.19 μM for PHD2. In acute myeloid leukemia (AML) cells, IOX5 can stabilize HIF-1α, inhibit cell proliferation, and induce apoptosis. It exhibits anti-leukemia activity.

PHD2-IN-6 (Example 89) is an inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 31.6 nM. This compound can stimulate the production of the gene encoding erythropoietin (EPO). PHD2-IN-6 is applicable in research on inflammatory diseases such as inflammatory bowel disease (IBD) and rheumatoid arthritis.

ZG-2686 is a potent and selective agonist of HIF-2α with an EC50 of 0.25 µM, demonstrating selectivity for PHD2. It binds to a specific internal cavity of HIF-2α, forming hydrogen bonds through structural water molecules, which stabilizes the HIF-2α/β heterodimer and enhances its transcriptional activity. The compound acts synergistically with Vadadustat to upregulate HIF-2α-dependent EPO gene expression both in vitro and in vivo. ZG-2686 is applicable for renal anemia research.

DS79540454 is an HIF-PHD2 inhibitor with an IC50 of 0.26 μM, and it is utilized in research related to renal anemia.

FG-2216 (YM-311) is a potent HIF-prolyl hydroxylase inhibitor for the PDH2 enzyme (IC50: 3.9 uM); orally bioavailable and induced reversible and significant Epo induction in vivo.

Molidustat (BAY 85-3934)(BAY-85-3934), an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH), stimulates erythropoietin (EPO) production and the formation of red blood cells.

JNJ-42041935 (HIF-PHD Inhibitor II) is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.

MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM).

TP-0463518 is a highly potent HIF prolyl hydroxylase (PHD) inhibitor (IC50s: 13 nM and 18 nM for human and rat PHD2, respectively).

HIF-PHD-IN-2 (compound 25) is a highly effective PHD inhibitor with IC50 values below 100 nM for PHD1, PHD2, and PHD3 [1].

Tert-butyl 4-[[1-[(4-chlorophenyl)methyl]-3-hydroxy-2-oxopyridin-4-yl]methyl]piperazine-1-carboxylate inhibit of human recombinant EGLN-1 as substrate after 20 mins by mass spectrophotometric analysis.

IOX4 is a potent PHD2 inhibitor (IC50 = 1.6 nM)

PHD2-IN-1, a potent and orally active HIF prolyl hydroxylase 2 (PHD2) inhibitor, exhibits an IC50 of 22.53 nM and is applicable in anemia research [1].