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Results for "

prolyl-hydroxylase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	HIF/HIF Prolyl-Hydroxylase (36) Apoptosis (2) Autophagy (1) Bacterial (1) Cannabinoid Receptor (1) DNA Methyltransferase (1) Ferroptosis (3) NO Synthase (1) Parasite (1) Phospholipase (1) PPAR (1) Reactive Oxygen Species (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (13) Infection (2) Inflammation/Immunology (8) Metabolic Disease (10) Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: HIF/HIF Prolyl-Hydroxylase Prolyl Endopeptidase (PREP) Tryptophan Hydroxylase Dopamine β-hydroxylase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-139287

M1002 1 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 .

HY-119351

BNS	HIF/HIF Prolyl-Hydroxylase	Others
BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor .

HY-W016409

Ethyl 3,4-dihydroxybenzoate 1 Publications Verification Protocatechuic acid ethyl ester	HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species NO Synthase Autophagy Apoptosis	Metabolic Disease Cancer
Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a *prolyl-hydroxylase* inhibitor found in the testa of peanut seeds. Ethyl 3,4-dihydroxybenzoate protects myocardium by activating NO synthase and generating mitochondrial ROS. Ethyl 3,4-dihydroxybenzoate induces cell autophagy and apoptosis in ESCC cells. Ethyl 3,4-dihydroxybenzoate is a collagen synthesis inhibitor and has a bone protecting-effect .

HY-13426

Roxadustat Maximum Cited Publications 36 Publications Verification FG-4592	HIF/HIF Prolyl-Hydroxylase Ferroptosis	Cancer
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 .

HY-13426S

Roxadustat-d5	HIF/HIF Prolyl-Hydroxylase Ferroptosis	Cancer
Roxadustat-d₅ is deuterium labeled Roxadustat. Roxadustat is an oral hypoxia-inducible factor prolyl-hydroxylase inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin[1].

HY-120110

IOX4 5 Publications Verification	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 .

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 .

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 .

HY-109057A

Enarodustat hydrochloride JTZ-951 hydrochloride; SAL0951 hydrochloride	HIF/HIF Prolyl-Hydroxylase	Metabolic Disease
Enarodustat hydrochloride is a potent and orally active HIF/HIF Prolyl-Hydroxylase inhibitor, with an EC₅₀ of 0.22 μM. Enarodustat hydrochloride has the potential for renal anemia treatment.

HY-13426R

Roxadustat (Standard)	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 .

HY-109057

Enarodustat 2 Publications Verification JTZ-951; SAL0951	HIF/HIF Prolyl-Hydroxylase	Metabolic Disease
Enarodustat is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC₅₀ of 0.22 μM. Enarodustat has the potential for renal anemia treatment.

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.

HY-17608

Daprodustat 10+ Cited Publications GSK1278863	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
Daprodustat (GSK1278863) is an orally active *hypoxia-inducible factor prolyl hydroxylase* (HIF-PH)** inhibitor being developed for the treatment of anemia associated with chronic kidney disease.

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.

HY-101449

Adaptaquin 1 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Metabolic Disease
Adaptaquin is an inhibitor of *hypoxia-inducible factor prolyl hydroxylase* 2 (HIF-PHD2), with an IC₅₀** of 2 μM. Adaptaquin can inhibit lipid peroxidation and maintain mitochondrial function .

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 .

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 .

HY-101277

Vadadustat 5+ Cited Publications PG-1016548; AKB-6548	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor . Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo .

HY-161660

DS44470011	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease Metabolic Disease
DS44470011 is a *hypoxia-inducing factor prolyl hydroxylase* (HIF-PHD)** inhibitor. DS44470011 has oral activity. DS44470011 promotes cell release of erythropoietin (EPO). DS44470011 can be used in the research of renal anemia .

HY-17608R

Daprodustat (Standard)	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
Daprodustat (Standard) is the analytical standard of Daprodustat. This product is intended for research and analytical applications. Daprodustat (GSK1278863) is an orally active *hypoxia-inducible factor prolyl hydroxylase* (HIF-PH)** inhibitor being developed for the treatment of anemia associated with chronic kidney disease.

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 pK_i values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.

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 .

HY-158341

IOX5	HIF/HIF Prolyl-Hydroxylase Apoptosis	Cancer
IOX5 is a selective prolyl hydroxylases (PHD) inhibitor. IOX5 stabilizes HIF-1α in AML cells, induces apoptosis, and upregulates BNIP3 expression. IOX5 compromises development and progression of acute myeloid leukemia .

HY-15641

FG-2216 3 Publications Verification 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 .

HY-163839

DS-1093a	HIF/HIF Prolyl-Hydroxylase	Metabolic Disease
DS-1093a is an orally active *hypoxia-inducible factor prolyl hydroxylase* (HIF-PHD)** inhibitor, with an EC₅₀ of 0.49 μM in Hep3B cell EPO production. DS-1093a can be used in the research of renal anemia .

HY-112678

TM6008	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
TM6008 is a potent and orally active prolyl hydroxylase (PHD) inhibitor. TM6008 chelats transition metal (copper) and inhibits the autoxidation of ascorbic acid with an IC₅₀ value is 0.57 μM. TM6008 exerts organ protection against ischemia in vivo and can be used for cerebrovascular disease research .

HY-15468

IOX2 5+ Cited Publications	HIF/HIF Prolyl-Hydroxylase	Cancer
IOX2 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 .

HY-15468A

IOX2 sodium	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease Cancer
IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC₅₀ of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases .

HY-129079A

TFMB-(S)-2-HG 1 Publications Verification	DNA Methyltransferase	Cancer
TFMB-(S)-2-HG is a potent inhibitor of the 5'-methylcytosine hydroxylase TET2. TFMB-(S)-2-HG also inhibits the EglN prolyl hydroxylases. TFMB-(S)-2-HG has the potential for the research of acute myeloid leukemia (AML) .

HY-112144

TP0463518	HIF/HIF Prolyl-Hydroxylase	Metabolic Disease
TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a K_i value of 5.3 nM for human PHD2. TP0463518 also inhibits human PHD1/PHD3 with IC₅₀s of 18 and 63 nM as well as monkey PHD2 with an IC₅₀ value of 22 nM .

HY-118543

TM6089	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia. Local administration of TM6089 enhances angiogenesis, and oral administration stimulates HIF activity in transgenic rats expressing a hypoxia-responsive reporter vector .

HY-113649

AKB-6899	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 .

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 .

HY-N7538

Dealanylalahopcin	Bacterial	Infection
Dealanylalahopcin is an antimicrobial agent that can be isolated from the culture filtrate of Streptomyces leucoderma subsp. ochraceus. Dealanylalahopcin can also be synthesized by enzymatic hydrolysis of alahopcin by microbial α-amino acid ester hydrolases. Dealanylalahopcin has weak antimicrobial activity against Gram-positive and Gram-negative bacteria and exhibits moderate inhibition of collagen prolyl hydroxylase .

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 .

HY-129502

Fibrostatin C P-23924C	Others	Others
Fibrostatin C is an orally active *prolyl hydroxylase* inhibitor that also inhibits collagen biosynthesis. Fibrostatin C also increases the number of cytoplasmic granules immunoreactive with antibodies to collagen I or III. Fibrostatin C inhibits the secretion of type I collagen in Tenon's capsule fibroblasts. Fibrostatin C is promising for research of the wound fibrotic response in the wound of glaucoma filtering surgery .

HY-44809

Izilendustat	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease Inflammation/Immunology
Izilendustat is a potent inhibitor of *prolyl hydroxylase* which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1) .

HY-44809A

Izilendustat hydrochloride	HIF/HIF Prolyl-Hydroxylase	Inflammation/Immunology Cancer
Izilendustat (hydrochloride) is a potent inhibitor of *prolyl hydroxylase* which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1) .

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 .

HY-P3100

Orfamide A	Parasite	Infection
Orfamide A is a major metabolite of insecticidal biosurfactant in Pseudomonas sp. F6 and has aphidicidal activity. Orfamide A can be used for aphid control in organic agriculture. Orfamide A exhibits dose-dependent mortality against aphids with an LC₅₀ value of 34.5 μg/mL .

HY-P10447

Plipastatin A1 Fengycin IX; SNA-60-367-3	Phospholipase	Inflammation/Immunology
Plipastatin A1 is a lipopeptide with enzyme inhibitory and immunosuppressive activities. Plipastatin A1 is found in Bacillus cereus and inhibits phospholipase A2 (PLA2), PLC, and PLD .

Cat. No.	Product Name

HY-L173

Anti-Ovarian Cancer Compound Library	2,010 compounds
Ovarian cancer is the most common cause of death in female genital malignancies, with the highest mortality rate in female genital malignancies. It is characterized by difficulty in detection in the early stage of the disease, high recurrence rate and poor prognosis. In fact, ovarian cancer includes many pathologic types. It is usually divided into epithelial ovarian cancer, malignant germ cell tumors and sex cord stromal tumors, of which epithelial ovarian cancer is the most dominant form. Clinical treatment of ovarian cancer prioritizes surgery combined with paclitaxel chemotherapy. However, due to the spread and drug resistance of tumor cells, the recurrence of ovarian cancer is high. In this case, combined with traditional methods, the development of new therapeutic agents can help to improve the treatment effect of ovarian cancer. MCE designs a unique collection of 2,010 compounds with definite or potential anti-ovarian cancer activity, which mainly targeting the main targets of ovarian cancer such as PARP, ATM/ATR, VEGFR and HIF/HIF Prolyl-Hydroxylase, etc. It is an essential tool for development and research of anti-ovarian compounds.

Anti-Ovarian Cancer Compound Library

2,010 compounds

Ovarian cancer is the most common cause of death in female genital malignancies, with the highest mortality rate in female genital malignancies. It is characterized by difficulty in detection in the early stage of the disease, high recurrence rate and poor prognosis. In fact, ovarian cancer includes many pathologic types. It is usually divided into epithelial ovarian cancer, malignant germ cell tumors and sex cord stromal tumors, of which epithelial ovarian cancer is the most dominant form. Clinical treatment of ovarian cancer prioritizes surgery combined with paclitaxel chemotherapy. However, due to the spread and drug resistance of tumor cells, the recurrence of ovarian cancer is high. In this case, combined with traditional methods, the development of new therapeutic agents can help to improve the treatment effect of ovarian cancer.

MCE designs a unique collection of 2,010 compounds with definite or potential anti-ovarian cancer activity, which mainly targeting the main targets of ovarian cancer such as PARP, ATM/ATR, VEGFR and HIF/HIF Prolyl-Hydroxylase, etc. It is an essential tool for development and research of anti-ovarian compounds.

HY-L045

Oxygen Sensing Compound Library	2,723 compounds
Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression. Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival. HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation. MCE offers a unique collection of 2,723 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Oxygen Sensing Compound Library

2,723 compounds

Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression.

Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival.

HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation.

MCE offers a unique collection of 2,723 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Cat. No.	Product Name	Target	Research Area

HY-P4755

*N-((RS)-2-Hydroxy-propyl)-Val-Leu-anilide*	Peptides	Others
N-((RS)-2-Hydroxy-propyl)-Val-Leu-anilide is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .