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Chromatin/Epigenetic HIF/HIF Prolyl-Hydroxylase

HIF/HIF Prolyl-Hydroxylase

HIF prolyl-hydroxylase is an enzyme involved in the HIF (Hypoxia-inducible factor) signalling pathways, and is the target for a set of therapeutic drugs called HIF prolyl-hydroxylase inhibitors.Hypoxia-inducible factor (HIF) is an evolutionarily conserved transcription factor[1] that allows the cell to respond physiologically to low concentrations of oxygen. A class of prolyl hydroxylases which act specifically on HIF has been identified; hydroxylation of HIF allows the protein to be targeted for degradation. HIF prolyl-hydroxylase has been targeted by a variety of inhibitors that aim to treat stroke, kidney disease, ischemia,anemia, and other important diseases. Clinically observed prolyl hydroxylase domain mutations, as in the case of erythrocytosis- and breast cancer-associated PHD2 mutations, affect its selectivity for its HIF substrate, which has important implication for drug design.
Cat No. product name
T1823 IOX 2 IOX2 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 ...
T2445 FG-2216 FG-2216 is a potent HIF-prolyl hydroxylase inhibitor for the PDH2 enzyme (IC50: 3.9 uM); orally bioavailable and induced reversible and significant Epo inductio...
T2652 Molidustat Molidustat(BAY-85-3934), an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH), stimulates erythropoietin (EPO) production and the formation of...
T3180 HIF-PHD Inhibitor II JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.
T4106 MK-8617 MK-8617 is an orally available HIF PHD1-3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM).
T4651 Vadadustat Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.
T5176 Desidustat Desidustat is an inhibitor of HIF hydroxylase.
T5392 TP0463518 TP-0463518 is a highly potent HIF prolyl hydroxylase (PHD) inhibitor (IC50s: 13 nM and 18 nM for human and rat PHD2, respectively).
T7880 IOX4 IOX4 is a potent PHD2 inhibitor (IC50 = 1.6 nM)
IOX 2
T1823CAS 931398-72-0
IOX2 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 ...
FG-2216
T2445CAS 223387-75-5
FG-2216 is a potent HIF-prolyl hydroxylase inhibitor for the PDH2 enzyme (IC50: 3.9 uM); orally bioavailable and induced reversible and significant Epo inductio...
Molidustat
T2652CAS 1154028-82-6
Molidustat(BAY-85-3934), an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH), stimulates erythropoietin (EPO) production and the formation of...
HIF-PHD Inhibitor II
T3180CAS 1193383-09-3
JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.
MK-8617
T4106CAS 1187990-87-9
MK-8617 is an orally available HIF PHD1-3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM).
Vadadustat
T4651CAS 1000025-07-9
Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.
Desidustat
T5176CAS 1616690-16-4
Desidustat is an inhibitor of HIF hydroxylase.
TP0463518
T5392CAS 1558021-37-6
TP-0463518 is a highly potent HIF prolyl hydroxylase (PHD) inhibitor (IC50s: 13 nM and 18 nM for human and rat PHD2, respectively).
IOX4
T7880CAS 1154097-71-8
IOX4 is a potent PHD2 inhibitor (IC50 = 1.6 nM)