HIF-1α stabilization

By Targets:	HIF/HIF Prolyl-Hydroxylase (12) Antibiotic (2) Apoptosis (3) Autophagy (3) Bacterial (2) E1/E2/E3 Enzyme (2) Ligands for E3 Ligase (1) MDM-2/p53 (1) Microtubule/Tubulin (2) NO Synthase (2) Parasite (2) Reactive Oxygen Species (ROS) (3) Reference Standards (2)
By Research Areas:	Cancer (10) Cardiovascular Disease (3) Infection (4) Inflammation/Immunology (2) Metabolic Disease (2) Neurological Disease (1)

Targets Recommended: HIF/HIF Prolyl-Hydroxylase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-121172

1,4-DPCA 1 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC₅₀ of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC₅₀ of 60 μM .

HY-B0413

Fenbendazole Maximum Cited Publications 9 Publications Verification	Parasite HIF/HIF Prolyl-Hydroxylase Microtubule/Tubulin Antibiotic	Infection Cancer
Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator *HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis*. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .

HY-19621

THS-044	HIF/HIF Prolyl-Hydroxylase	Cancer
THS-044 is a modulator of the formation of the HIF2α/ARNT heterodimer. THS-044 binding stabilizes the HIF2α PAS-B folded state (K_D = 2 μM), for regulating HIF2 activity in endogenous and pathological settings, and does not bind to HIF1α or ARNT PAS-B. THS-044 can be used for the study of diseases related to hypoxia .

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 .

HY-156106

VHL-IN-1	HIF/HIF Prolyl-Hydroxylase Ligands for E3 Ligase E1/E2/E3 Enzyme	Cancer
VHL-IN-1 (Compound 30) is an E3 ligase VHL inhibitor with a K_d value of 37 nM. VHL-IN-1 blocks VHL-mediated ubiquitination and degradation of *HIF-1α. VHL-IN-1 stabilizes* the protein levels of *HIF-1α* and hydroxylated *HIF-1α, and induces the transcriptional activity of HIF-1α*. VHL-IN-1 can be used for PROTAC development. VHL-IN-1 is applicable for cancer research .

HY-44809

Izilendustat	HIF/HIF Prolyl-Hydroxylase Bacterial	Cardiovascular Disease Infection Inflammation/Immunology
Izilendustat is a potent prolyl hydroxylase inhibitor. Izilendustat competitively inhibits HIFPH2 activity, blocks *HIF-1α* degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia .

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 .

HY-15893G

DMOG Dimethyloxallyl Glycine	Autophagy HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
DMOG (GMP) is the GMP level of DMOG (HY-15893). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DMOG (GMP) is a HIF-1α stabilizer. DMOG (GMP) promotes the osteogenic, angiogenic, and chondrogenic differentiation of stem cells by stabilizing the expression of HIF-1α. DMOG (GMP) can enhance the osteogenic and angiogenic differentiation potential of stem cells, thereby improving bone regeneration in bone defects. DMOG (GMP) can be used in the research of bone defect repair, vascularized bone regeneration, and the treatment of bone-related diseases (such as osteoporosis and femoral head necrosis) .

HY-B0413R

Fenbendazole (Standard)	Reference Standards Parasite HIF/HIF Prolyl-Hydroxylase Microtubule/Tubulin Antibiotic	Infection
Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator *HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis*. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .

HY-158685

RG7112D	MDM-2/p53	Cancer
RG7112D is a potent MDM2 inhibitor with IC₅₀s of 11 nM and >10000 nM and for MDM2-p53 and VHL-HIF1α by binding HTRF assay, respectively. RG7112D is coupled by an amide bond to VHL-Amine, resulting in a bi-functional molecule, YX-02-030. YX-02-03, a MDM2-PROTAC, potently inhibits MDM2-p53 binding (HTRF IC₅₀=63nM). RG7112D can stabilize MDM2 protein and increase p53 protein levels .

HY-44809A

Izilendustat hydrochloride	HIF/HIF Prolyl-Hydroxylase Bacterial	Cardiovascular Disease Infection Inflammation/Immunology
Izilendustat hydrochloride is a potent prolyl hydroxylase inhibitor. Izilendustat hydrochloride competitively inhibits HIFPH2 activity, blocks *HIF-1α* degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat hydrochloride can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat hydrochloride can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia .

HY-W778057

Ethyl 3,4-Dihydroxybenzoate-13C3 Protocatechuic acid ethyl ester-¹³C₃	Reactive Oxygen Species (ROS)	Cancer
Ethyl 3,4-Dihydroxybenzoate- ¹³C₃ (Protocatechuic acid ethyl ester- ¹³C₃) is the ¹³C-labeled Ethyl 3,4-dihydroxybenzoate (HY-W016409). 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 .

HY-W016409R

Ethyl 3,4-dihydroxybenzoate (Standard) Protocatechuic acid ethyl ester (Standard)	Reference Standards HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species (ROS) NO Synthase Autophagy Apoptosis	Metabolic Disease Cancer
Ethyl 3,4-dihydroxybenzoate (Standard) (Protocatechuic acid ethyl ester (Standard)) is the analytical standard of Ethyl 3,4-dihydroxybenzoate (HY-W016409). This product is intended for research and analytical applications. 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 .

HY-183638

T7117	E1/E2/E3 Enzyme HIF/HIF Prolyl-Hydroxylase	Neurological Disease Cancer
T7117 is a TRIM25-HIF-1α inhibitor. T7117 disrupts the interaction between TRIM25-HIF-1α. T7117 can be used for the research of glioblastoma .

Cat. No.	Product Name

HY-L045

Oxygen Sensing Compound Library	4,029 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 4,029 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

4,029 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 4,029 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	Type

HY-15893G

DMOG Dimethyloxallyl Glycine	Fluorescent Dyes
DMOG (GMP) is the GMP level of DMOG (HY-15893). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DMOG (GMP) is a HIF-1α stabilizer. DMOG (GMP) promotes the osteogenic, angiogenic, and chondrogenic differentiation of stem cells by stabilizing the expression of HIF-1α. DMOG (GMP) can enhance the osteogenic and angiogenic differentiation potential of stem cells, thereby improving bone regeneration in bone defects. DMOG (GMP) can be used in the research of bone defect repair, vascularized bone regeneration, and the treatment of bone-related diseases (such as osteoporosis and femoral head necrosis) .

DMOG

Dimethyloxallyl Glycine

Fluorescent Dyes

DMOG (GMP) is the GMP level of DMOG (HY-15893). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DMOG (GMP) is a HIF-1α stabilizer. DMOG (GMP) promotes the osteogenic, angiogenic, and chondrogenic differentiation of stem cells by stabilizing the expression of HIF-1α. DMOG (GMP) can enhance the osteogenic and angiogenic differentiation potential of stem cells, thereby improving bone regeneration in bone defects. DMOG (GMP) can be used in the research of bone defect repair, vascularized bone regeneration, and the treatment of bone-related diseases (such as osteoporosis and femoral head necrosis) .

Cat. No.	Product Name	Type

HY-15893G

DMOG Dimethyloxallyl Glycine	Biochemical Assay Reagents
DMOG (GMP) is the GMP level of DMOG (HY-15893). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DMOG (GMP) is a HIF-1α stabilizer. DMOG (GMP) promotes the osteogenic, angiogenic, and chondrogenic differentiation of stem cells by stabilizing the expression of HIF-1α. DMOG (GMP) can enhance the osteogenic and angiogenic differentiation potential of stem cells, thereby improving bone regeneration in bone defects. DMOG (GMP) can be used in the research of bone defect repair, vascularized bone regeneration, and the treatment of bone-related diseases (such as osteoporosis and femoral head necrosis) .

DMOG

Dimethyloxallyl Glycine

Biochemical Assay Reagents

DMOG (GMP) is the GMP level of DMOG (HY-15893). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DMOG (GMP) is a HIF-1α stabilizer. DMOG (GMP) promotes the osteogenic, angiogenic, and chondrogenic differentiation of stem cells by stabilizing the expression of HIF-1α. DMOG (GMP) can enhance the osteogenic and angiogenic differentiation potential of stem cells, thereby improving bone regeneration in bone defects. DMOG (GMP) can be used in the research of bone defect repair, vascularized bone regeneration, and the treatment of bone-related diseases (such as osteoporosis and femoral head necrosis) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W016409

Ethyl 3,4-dihydroxybenzoate 1 Publications Verification Protocatechuic acid ethyl ester	Arachis hypogaea L. Classification of Application Fields Leguminosae Phenols Polyphenols Metabolic Disease Plants Disease Research Fields Source Classification	HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species (ROS) NO Synthase Autophagy Apoptosis
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 .

HY-W016409R

Ethyl 3,4-dihydroxybenzoate (Standard) Protocatechuic acid ethyl ester (Standard)	Structural Classification Arachis hypogaea L. Leguminosae Phenols Polyphenols Plants Source Classification	Reference Standards HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species (ROS) NO Synthase Autophagy Apoptosis
Ethyl 3,4-dihydroxybenzoate (Standard) (Protocatechuic acid ethyl ester (Standard)) is the analytical standard of Ethyl 3,4-dihydroxybenzoate (HY-W016409). This product is intended for research and analytical applications. 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 .

Cat. No.	Product Name	Chemical Structure

HY-W778057

Ethyl 3,4-Dihydroxybenzoate-13C3
Ethyl 3,4-Dihydroxybenzoate- ¹³C₃ (Protocatechuic acid ethyl ester- ¹³C₃) is the ¹³C-labeled Ethyl 3,4-dihydroxybenzoate (HY-W016409). 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-13C3

Ethyl 3,4-Dihydroxybenzoate- ¹³C₃ (Protocatechuic acid ethyl ester- ¹³C₃) is the ¹³C-labeled Ethyl 3,4-dihydroxybenzoate (HY-W016409). 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 .

Targets Recommended: HIF/HIF Prolyl-Hydroxylase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15893G

DMOG Dimethyloxallyl Glycine	Autophagy HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
DMOG (GMP) is the GMP level of DMOG (HY-15893). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DMOG (GMP) is a HIF-1α stabilizer. DMOG (GMP) promotes the osteogenic, angiogenic, and chondrogenic differentiation of stem cells by stabilizing the expression of HIF-1α. DMOG (GMP) can enhance the osteogenic and angiogenic differentiation potential of stem cells, thereby improving bone regeneration in bone defects. DMOG (GMP) can be used in the research of bone defect repair, vascularized bone regeneration, and the treatment of bone-related diseases (such as osteoporosis and femoral head necrosis) .

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HIF-1α stabilization

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Biochemical Assay Reagents

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Isotope-Labeled Compounds

GMP Molecules

Natural
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