hif-phd2

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

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.

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.

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.

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.

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].