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.
Inhibitors Catalog Download
产品编号 产品名称
T9627 PHD-1-IN-1 PHD-1-IN-1 is a potent inhibitor of hypoxia-inducible factor prolylhydroxylase domain-1 (PHD-1) enzyme(IC50 = 0.034 μM).
T001-00000002 Izilendustat 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 m...
T7880 IOX4 IOX4 is a potent PHD2 inhibitor (IC50 = 1.6 nM)
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).
T5176 Desidustat Desidustat is an inhibitor of HIF hydroxylase.
T6S1315 Oroxylin A 1. Oroxylin A has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting th...
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).
T1823 IOX2 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 n...
T2941 Glucosamine hydrochloride Glucosamine is commonly used as a treatment for osteoarthritis, although its acceptance as a medical therapy varies.
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 induction...
T3180 JNJ-42041935 JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.
T2652 Molidustat Molidustat(BAY-85-3934), an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH), stimulates erythropoietin (EPO) production and the formation of ...
PHD-1-IN-1
T9627CAS 2009343-14-8
PHD-1-IN-1 is a potent inhibitor of hypoxia-inducible factor prolylhydroxylase domain-1 (PHD-1) enzyme(IC50 = 0.034 μM).
Izilendustat
T001-00000002CAS 1303512-02-8
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 m...
IOX4
T7880CAS 1154097-71-8
IOX4 is a potent PHD2 inhibitor (IC50 = 1.6 nM)
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).
Desidustat
T5176CAS 1616690-16-4
Desidustat is an inhibitor of HIF hydroxylase.
Oroxylin A
T6S1315CAS 480-11-5
1. Oroxylin A has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting th...
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).
IOX2
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 n...
Glucosamine hydrochloride
T2941CAS 66-84-2
Glucosamine is commonly used as a treatment for osteoarthritis, although its acceptance as a medical therapy varies.
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 induction...
JNJ-42041935
T3180CAS 1193383-09-3
JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.
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 ...
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