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PHD inhibitor

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67

Inhibitors & Agonists

4

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13426
    Roxadustat
    Maximum Cited Publications
    59 Publications Verification

    FG-4592

    		 HIF/HIF Prolyl-Hydroxylase Ferroptosis Infection Cancer
    Roxadustat is an orally active hypoxia-inducible factor prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin .
    Roxadustat
  • HY-15468
    IOX2
    15+ Cited Publications

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    IOX2, a chemical probe, is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 can be used in the study of thrombotic diseases .
    IOX2
  • HY-12654
    Molidustat
    5+ Cited Publications

    BAY 85-3934

    		 HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia .
    Molidustat
  • HY-120110
    IOX4
    5+ Cited Publications

    		 HIF/HIF Prolyl-Hydroxylase Neurological Disease Inflammation/Immunology
    IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2 .
    IOX4
  • HY-12832
    JNJ-42041935

    		HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    JNJ-42041935 is a potent, competitive and selective inhibitor of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.
    JNJ-42041935
  • HY-101023
    MK-8617
    3 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.
    MK-8617
  • HY-112144
    TP0463518
    1 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Metabolic Disease Inflammation/Immunology
    TP0463518 is an orally active, competitive pan-inhibitor of hypoxia-inducible factor prolyl hydroxylases PHD1/2/3. TP0463518 competitively inhibits human PHD1 (IC50=18 nM), PHD2 (Ki=5.3 nM), and PHD3 (IC50=63 nM), and targets monkey PHD2 with an IC50 of 22 nM. TP0463518 inhibits PHD-catalyzed hydroxylation to stabilize HIFα, thereby upregulating erythropoietin (EPO) expression and enhancing intestinal iron absorption (such as increased DMT-1 and dCYTb expression), improving anemia. TP0463518 is mainly used for the research of renal anemia and inflammatory anemia .
    TP0463518
  • HY-N1477
    Dencichine

    Dencichin; ODAP

    		 HIF/HIF Prolyl-Hydroxylase Neurological Disease
    Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity.
    Dencichine
  • HY-W016409
    Ethyl 3,4-dihydroxybenzoate
    1 Publications Verification

    Protocatechuic acid ethyl ester

    		 HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species (ROS) NO Synthase Autophagy Apoptosis Metabolic Disease Cancer
    Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema .
    Ethyl 3,4-dihydroxybenzoate
  • HY-101449
    Adaptaquin
    2 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species (ROS) Neurological Disease Metabolic Disease Inflammation/Immunology
    Adaptaquin is a BBB-penetrable HIF-PHDs inhibitor. Adaptaquin has anti-inflammatory and neuroprotective effects. Adaptaquin can effectively inhibit lipid peroxidation, maintain mitochondrial function, and reduce neuronal death. Adaptaquin can be used in the research of nervous system diseases such as Parkinson's disease .
    Adaptaquin
  • HY-15641
    FG-2216
    5+ Cited Publications

    IOX3; YM311

    		 HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo .
    FG-2216
  • HY-12315
    N-Oxalylglycine

    N-Oxaloglycine

    		 Histone Demethylase HIF/HIF Prolyl-Hydroxylase Cancer
    N-Oxalylglycine (N-Oxaloglycine) is a Jumonji C-domain-containing histone lysine demethylase inhibitor. N-Oxalylglycine inhibits JMJD2A, JMJD2C and JMJD2D. N-Oxalylglycine also inhibits HIF prolylhydroxylase domain-1 (PHD-1) and PHD-2, with an IC50 of 2.1 μM and 5.6 μM, respectively .
    N-Oxalylglycine
  • HY-158341
    IOX5

    		HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    IOX5 is a selective prolyl hydroxylase (PHD) inhibitor with an IC50 of 0.19 μM for PHD2. IOX5 stabilizes HIF-1α in acute myeloid leukemia (AML) cells, inhibits cell proliferation and induces apoptosis. IOX5 has anti-leukemia activity .
    IOX5
  • HY-139287
    M1002
    2 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors .
    M1002
  • HY-123422
    GSK360A

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) .
    GSK360A
  • HY-113649
    AKB-6899
    2 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects .
    AKB-6899
  • HY-170522
    ISM012-042

    		HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases .
    ISM012-042
  • HY-141703A
    DC-BPi-11 hydrochloride

    		Epigenetic Reader Domain Cancer
    DC-BPi-11 hydrochloride is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC50 value of 698 nM. DC-BPi-11 hydrochloride shows remarkable inhibition against leukemia cell proliferation .
    DC-BPi-11 hydrochloride
  • HY-157891
    JBC117

    		Apoptosis Cancer
    JBC117 is a novel anticancer lead compound targeting Pygo2 PHD. JBC117 can effectively antagonize the cell effect of β-catenin-dependent activity and inhibit the migration and invasion of cancer cells. JBC117 can induce apoptosis .
    JBC117
  • HY-128872
    Etrinabdione

    EHP-101; VCE-​004.8

    		 PPAR Cannabinoid Receptor HIF/HIF Prolyl-Hydroxylase Metabolic Disease Inflammation/Immunology
    Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity .
    Etrinabdione
  • HY-168533
    ZG-2305

    		HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    ZG-2305 is a potent, orally active and selective factor inhibiting hypoxia-inducible factor (FIH) inhibitor with Ki values of 79.6, 2786 nM for FIH, PHD2, respectively. ZG-2305 increases the expression of EGLN3 gene. ZG-2305 decreases the cellular triglycerides levels and reduces lipid accumulation. ZG-2305 has the potential for the research of obesity and fatty liver disease .
    ZG-2305
  • HY-136300
    PHD-1-IN-1

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease Inflammation/Immunology
    PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe 2+ ion and induces the formation of an "Arg367-out" pocket .
    PHD-1-IN-1
  • HY-119351
    BNS

    		HIF/HIF Prolyl-Hydroxylase Others
    BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor .
    BNS
  • HY-126299
    NVS-BPTF-1

    		Epigenetic Reader Domain Others
    NVS-BPTF-1, a chemical probe, is a selective inhibitor for bromodomain and PHD finger containing transcription factor (BPTF), with KD of 71 nM .
    NVS-BPTF-1
  • HY-141703
    DC-BPi-11

    		Epigenetic Reader Domain Cancer
    DC-BPi-11 is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC50 value of 698 nM. DC-BPi-11 shows remarkable inhibition against leukemia cell proliferation .
    DC-BPi-11
  • HY-151364
    HDAC6/8/BRPF1-IN-1

    		HDAC Cancer
    HDAC6/8/BRPF1-IN-1 is a dual inhibitor of both HDAC6/8 and the bromodomain and PHD finger containing protein 1 (BRPF1). HDAC6/8/BRPF1-IN-1 has inhibitory activity for HDAC1, HDAC6 and HDAC8 with IC50 values of 797 nM, 344 nM and 908 nM, respectively. HDAC6/8/BRPF1-IN-1 has inhibitory activity for BRPF1 with an Kd value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer .
    HDAC6/8/BRPF1-IN-1
  • HY-112441
    Prolyl Hydroxylase inhibitor 1

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM . Antianemia agent .
    Prolyl Hydroxylase inhibitor 1
  • HY-145431
    (S)-GSK1379725A

    		Epigenetic Reader Domain Parasite Infection
    (S)-GSK1379725A (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. (S)-GSK1379725A shows to be selective for BPTF over BRD4 bromodomain. (S)-GSK1379725A shows antimalarial activity .
    (S)-GSK1379725A
  • HY-W747868
    Molidustat sodium

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia .
    Molidustat sodium
  • HY-N6030
    (Rac)-Dencichine

    (Rac)-Dencichin; (Rac)-ODAP

    		 HIF/HIF Prolyl-Hydroxylase Others
    (Rac)-Dencichine ((Rac)-Dencichin) is the racemate of Dencichin. Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity .
    (Rac)-Dencichine
  • HY-403658
    IOX2-NH2

    		Drug Derivative HIF/HIF Prolyl-Hydroxylase Others
    IOX2-NH2 (example 115) is a derivative of IOX2 (HY-15468). IOX2 is a chemical probe, and a specific prolyl hydroxylase-2 (PHD2) inhibitor .
    IOX2-NH2
  • HY-13426R
    Roxadustat (Standard)

    FG-4592 (Standard)

    		 Reference Standards HIF/HIF Prolyl-Hydroxylase Ferroptosis Cancer
    Roxadustat (Standard) is the analytical standard of Roxadustat. This product is intended for research and analytical applications. Roxadustat is an orally active hypoxia-inducible factor (HIF) prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin .
    Roxadustat (Standard)
  • HY-15641R
    FG-2216 (Standard)

    IOX3 (Standard); YM311 (Standard)

    		 HIF/HIF Prolyl-Hydroxylase Reference Standards Metabolic Disease
    FG-2216 (Standard) is the analytical standard of FG-2216. This product is intended for research and analytical applications. FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo .
    FG-2216 (Standard)
  • HY-163148
    PHD-IN-3

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    PHD-IN-3 (Compound 15) is an orally active PHD inhibitor. PHD-IN-3 can be used in the study of anemia associated with chronic kidney disease .
    PHD-IN-3
  • HY-170917
    PHD2-IN-4

    		HIF/HIF Prolyl-Hydroxylase
    PHD2-IN-4 (compound 1) is a PHD2 inhibitor. PHD2-IN-4 inhibits PHD2 with an IC50 of 4 nM. PHD2-IN-4 is potential for chronic kidney disease research .
    PHD2-IN-4
  • HY-15692
    PHD2-IN-3

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    PHD2-IN-3 (compound 2) is a PHD2 inhibitor. PHD2-IN-3 can be used for study of anemia .
    PHD2-IN-3
  • HY-139993
    HIF-PHD-IN-2

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    HIF-PHD-IN-2 (compound 25) is a potent PHD inhibitor with IC50s of <100 nM for PHD1, PHD2 and PHD3, respectively .
    HIF-PHD-IN-2
  • HY-176408
    PHD2-IN-5

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    PHD2-IN-5 (compound 22) is a potent PHD2 inhibitor with an IC50 of 0.82 μM. PHD2-IN-5 can be used in the study of renal anemia .
    PHD2-IN-5
  • HY-162438
    PHD2-IN-2

    		HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    PHD2-IN-2 (Compound 12) is a PHD2 inhibitor, with an IC50 of 34.3 nM. PHD2-IN-2 has high erythropoietin (EPO) inducing activity, with an EC50 of 6.79 μM. PHD2-IN-2 can be used for the research of anemia, ischemia, and hypoxia .
    PHD2-IN-2
  • HY-155009
    PHD2-IN-1

    		HIF/HIF Prolyl-Hydroxylase Others
    PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research .
    PHD2-IN-1
  • HY-177271
    PHD2-IN-6

    		HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    PHD2-IN-6 (Example 89) is a HIF prolyl hydroxylase 2 (PHD2) inhibitor with an IC50 of 31.6  nM. PHD2-IN-6 stimulates encoding erythropoietin (EPO) production. PHD2-IN-6 can be used for inflammatory diseases like inflammatory bowel disease (IBD) and rheumatoid arthritis research .
    PHD2-IN-6
  • HY-144332
    PHD2/HDACs-IN-1

    		HDAC HIF/HIF Prolyl-Hydroxylase Cancer
    PHD2/HDACs-IN-1 is a potent PHD2/HDACs hybrid inhibitor (IC50s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2, HDAC1, HDAC2 and HDAC6, respectively). PHD2/HDACs-IN-1 is a low-toxicity renoprotective agent for research of cisplatin-induced acute kidney injury (AKI) .
    PHD2/HDACs-IN-1
  • HY-131346
    HIF-PHD-IN-1

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia .
    HIF-PHD-IN-1
  • HY-124133
    JNJ-42905343

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    JNJ-42905343 is an orally active and highly selective prolyl hydroxylase (PHD1/2/3) inhibitor with pKI values of 8.07, 7.48 and 7.27 for PHD1, PHD2 and PHD3, respectively. JNJ-42905343 is promising for research of functional iron deficiency (FID) and anemia of chronic disease (ACD) .
    JNJ-42905343
  • HY-172257
    HIF-PHD-IN-4

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-PHD-IN-4 (Compound 13) is an orally active PHD2 inhibitor with an IC50 of 100 nM. HIF-PHD-IN-4 can effectively enhance the mobilization of hematopoietic stem cells induced by G-CSF in mice at a dose of 2 mg/kg. HIF-PHD-IN-4 is suitable for research in the field of tumor therapy .
    HIF-PHD-IN-4
  • HY-156526
    PHD-IN-1

    		HIF/HIF Prolyl-Hydroxylase Others
    PHD-IN-1 (compound 80) is a potent inhibitor of PHD2，with an IC50 value of ≤5 nM. PHD-IN-1 shows EC50s of 2.5 μM in EPO Elisa assay both in Caco2-HIFla-HiBiT-clone-1 cells and Hep3B cells，respectively .
    PHD-IN-1
  • HY-12315R
    N-Oxalylglycine (Standard)

    N-Oxaloglycine (Standard)

    		 Histone Demethylase HIF/HIF Prolyl-Hydroxylase Reference Standards Cancer
    N-Oxalylglycine (Standard) is the analytical standard of N-Oxalylglycine. This product is intended for research and analytical applications. N-Oxalylglycine (N-Oxaloglycine) is a Jumonji C-domain-containing histone lysine demethylase inhibitor. N-Oxalylglycine inhibits JMJD2A, JMJD2C and JMJD2D. N-Oxalylglycine also inhibits HIF prolylhydroxylase domain-1 (PHD-1) and PHD-2, with an IC50 of 2.1 μM and 5.6 μM, respectively .
    N-Oxalylglycine (Standard)
  • HY-170914
    JPHM-2-167

    		HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    JPHM-2-167 (Compound 11) is a selective PHD (prolyl hydroxylase domain enzyme) inhibitor. JPHM-2-167 inhibits PHD2, PHD3 with IC50s of 0.253 μM and 3.95 μM, respectively. JPHM-2-167 can be used for chronic kidney disease .
    JPHM-2-167
  • HY-12654R
    Molidustat (Standard)

    BAY 85-3934 (Standard)

    		 HIF/HIF Prolyl-Hydroxylase Reference Standards Cardiovascular Disease
    Molidustat (Standard) is the analytical standard of Molidustat. This product is intended for research and analytical applications. Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia .
    Molidustat (Standard)
  • HY-170915
    DDO-3055

    		HIF/HIF Prolyl-Hydroxylase Others
    DDO-3055 is an orally active PHD2 inhibitor that can be used in the research of anemia associated with chronic kidney disease .
    DDO-3055

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