PHD2

PhD2, an antimicrobial peptide originating from monkey leukocytes, exhibits efficacy against bacteria and the fungus Candida albicans [1].

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).

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).

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)

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

PHD2/HDACs-IN-1 is a potent mixed inhibitor of PHD2/HDACs, acting on PHD2 (IC50: 1.15 μM), HDAC1 (IC50: 19.75 μM), HDAC2 (IC50: 26.60 μM), and HDAC16 (IC50: 15.98 μM). HDACs-IN-1 is a low toxicity nephroprotective agent suitable for studies of cisplatin-induced acute kidney injury (AKI).

PHD2-IN-4 (compound 1) is an inhibitor of PHD2, with an IC50 of 4 nM. It is utilized in research related to chronic kidney disease.

PHD2-IN-5 (compound 22) is a potent inhibitor of PHD2, with an IC50 of 0.82 μM. It is applicable for research into renal anemia.

PHD2-IN-2 (Compound 12) is a PHD2 inhibitor with an IC50 of 34.3 nM. It demonstrates significant erythropoietin (EPO) induction activity with an EC50 of 6.79 μM. This compound is applicable in research related to anemia, ischemia, and hypoxia.

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.

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].

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-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.

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

ISM012-042 is an orally active inhibitor of PHD1 and PHD2, with IC50 values of 1.9 and 2.5 nM, respectively. At a concentration of 2.5 μM, ISM012-042 protects Caco-2 cells from DSS-induced barrier damage. Additionally, in LPS-induced bone marrow-derived dendritic cells (BMDC) from mice, ISM012-042 exhibits anti-inflammatory properties by dose-dependently reducing the expression of IL-12 subunit IL-12p35 and TNF. It also restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 is useful for studying intestinal mucosal repair and immune disorders.

DDO-3055 is an orally active PHD2 inhibitor utilized in studies related to anemia associated with chronic kidney disease.

PHM-2-167 (Compound 11) is a selective inhibitor of the prolyl hydroxylase domain enzyme (PHD). It inhibits PHD2 and PHD3 with IC50 values of 0.253 μM and 3.95 μM, respectively. PHM-2-167 is applicable for research in chronic kidney disease.

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.