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Results for "

HIF-1alpha

" in MedChemExpress (MCE) Product Catalog:

By Targets:	HIF/HIF Prolyl-Hydroxylase (125) ADC Payload (3) Akt (20) Aldehyde Dehydrogenase (ALDH) (1) AMPK (1) Amyloid-β (2) Antibiotic (22) AP-1 (1) Apoptosis (48) ATP Synthase (1) Autophagy (19) Bacterial (19) Bcl-2 Family (3) Beclin1 (3) c-Met/HGFR (1) Calcium Channel (7) Cannabinoid Receptor (2) Caspase (4) CDK (3) Cholecystokinin Receptor (3) Cholinesterase (ChE) (2) COX (2) DNA/RNA Synthesis (1) Drug Isomer (1) E1/E2/E3 Enzyme (2) E3 Ligase Ligand-Linker Conjugates (2) Endogenous Metabolite (7) Ephrin Receptor (3) Epigenetic Reader Domain (2) ERK (3) FAK (1) Fluorescent Dye (2) Fungal (6) Glutathione Peroxidase (2) Histone Acetyltransferase (2) Histone Methyltransferase (2) HIV (4) HSP (5) HSV (1) IDE (1) IKK (1) Influenza Virus (3) Interleukin Related (12) Isotope-Labeled Compounds (9) JNK (5) Keap1-Nrf2 (6) Lactate Dehydrogenase (2) Ligands for E3 Ligase (3) Malate Dehydrogenase (MDH) (1) MDM-2/p53 (14) MEK (1) MicroRNA (5) Microtubule/Tubulin (6) Mitochondrial Metabolism (2) MMP (5) Monoamine Oxidase (1) Monocarboxylate Transporter (2) mTOR (6) Natriuretic Peptide Receptor (NPR) (1) NF-κB (9) NO Synthase (6) NOD-like Receptor (NLR) (1) Notch (1) Oxidative Phosphorylation (2) p38 MAPK (3) Parasite (8) PARP (2) PD-1/PD-L1 (4) PDHK (1) PI3K (5) Potassium Channel (7) PPAR (2) PROTACs (2) Protein Arginine Deiminase (1) Proteolytic Enzyme (1) Proton Pump (1) Pyroptosis (1) Pyruvate Kinase (2) Raf (1) Ras (2) Reactive Oxygen Species (ROS) (23) Reference Standards (15) SARS-CoV (2) Small Interfering RNA (siRNA) (3) SOD (2) Src (1) STAT (8) Survivin (1) TAM Receptor (1) TNF Receptor (7) Topoisomerase (3) Trk Receptor (1) VEGFR (16) Xanthine Oxidase (4)
By Research Areas:	Cancer (139) Cardiovascular Disease (24) Infection (36) Inflammation/Immunology (41) Metabolic Disease (23) Neurological Disease (24)
Oligonucleotides:	Rat Pre-designed siRNA Sets (1) Mouse Pre-designed siRNA Sets (1) Human Pre-designed siRNA Sets (1) Antisense Oligonucleotides (2) Cholesterol (1) siRNAs (3)

170

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Antibodies

Oligonucleotides

HIF-1 alpha (556-574)	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
HIF-1 alpha (556-574) is a short hypoxia-inducible factor-1 (HIF-1) 19 residues fragment. HIF-1 functions as master regulator of response to oxygen homeostasis ^[1].

Oligomycin 75+ Cited Publications	Oxidative Phosphorylation ATP Synthase Fungal Antibiotic	Infection Cancer
Oligomycin, an antifungal antibiotic, is an inhibitor of H ⁺-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells ^[1] .

HIF-1α-IN-2 hydrochloride 3 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-2 hydrochloride is an effective *HIF-1α* inhibitor with anticancer potencies (IC₅₀s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 hydrochloride suppresses HIF-1α expression by blocking transcription and protein translation ^[1].

HIF-1α-IN-2 3 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-2 is an effective *HIF-1α* inhibitor with anticancer potencies (IC₅₀s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation ^[1].

*PROTAC HIF-1α* degrader-1**	PROTACs Apoptosis HIF/HIF Prolyl-Hydroxylase	Cancer
PROTAC HIF-1α degrader-1 (compound V2) is a potent hypoxia-inducible factor-1α (HIF-1α) PROTAC degrader with an IC₅₀ value of 7.54 µM. PROTAC HIF-1α degrader-1 shows anti-proliferative activity. PROTAC HIF-1α degrader-1 decreases the HIF-1α protein expression. PROTAC HIF-1α degrader-1 induces apoptosis. (Pink: ligand for target protein (HY-111387); black: linker (HY-W013731); Blue: E3 ligase ligand (HY-112078)) ^[1].

HIF-1α-IN-5	HIF/HIF Prolyl-Hydroxylase Monoamine Oxidase	Cancer
HIF-1α-IN-5 is a *HIF-1α* inhibitor with an IC₅₀ value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer ^[1].

HIF-1 alpha (556-574) TFA	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
HIF-1 alpha (556-574) TFA is a short hypoxia-inducible factor-1 (HIF-1) 19 residues fragment. HIF-1 functions as master regulator of response to oxygen homeostasis ^[1].

HIF-1α-IN-6	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-6 (compound 3s) is a *HIF-1α* inhibitor with IC₅₀ values of 0.6 and 53.3 nM observed in MiaPaCa-2 and MDA-MB-231 cells. HIF-1α-IN-6 can inhibit HIF-1α expression by decreasing the level of HIF-1α mRNA ^[1].

HIF-1α-IN-7	HIF/HIF Prolyl-Hydroxylase	Neurological Disease
HIF-1α-IN-7 (Compound D13) is a potent *HIF-1α* inhibitor. HIF-1α-IN-7 has neuroprotective activity. HIF-1α-IN-7 can be used in Alzheimer's disease research ^[1].

HIF-1α-IN-3	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-3 (Compound (S)-3f) is a hypoxia-selective *HIF-1α* inhibitor. HIF-1α-IN-3 shows strong antiestrogenic potency ^[1].

HIF-1α-IN-4	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-4 is a *HIF-1α* inhibitor with an IC₅₀ value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer ^[1].

HIF-1α-IN-8	HIF/HIF Prolyl-Hydroxylase IKK NF-κB Apoptosis Reactive Oxygen Species (ROS)	Inflammation/Immunology
HIF-1α-IN-8 is an orally active *HIF-1α* inhibitor, with an IC₅₀ of 2.02 μM. HIF-1α-IN-8 significantly suppresses the expression of inflammation factors of IL-6 and NO, reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells. HIF-1α-IN-8 inhibits *HIF-1α/IKKα/NF-κB* signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins. HIF-1α-IN-8 reduces brain water content and oxidative stress level in mice with high altitude cerebral edema (HACE) model. HIF-1α-IN-8 can be used for the study of high altitude cerebral edema (HACE) ^[1].

LW6 50+ Cited Publications HIF-1α inhibitor; LW8	HIF/HIF Prolyl-Hydroxylase Apoptosis	Cancer
LW6 (HIF-1α inhibitor) is a novel *HIF-1* inhibitor with an IC₅₀ value of 4.4 μM, and it is also an inhibitor of MDH2. LW6 decreases *HIF-1α* protein expression without affecting HIF-1β expression.

*NF-κB/HIF-1α-IN-1*	NF-κB HIF/HIF Prolyl-Hydroxylase Keap1-Nrf2	Cancer
NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and *HIF-1α, while simultaneously inducing the activation of Nrf2* ^[1].

ENMD-1198 IRC-110160	Microtubule/Tubulin HIF/HIF Prolyl-Hydroxylase STAT	Cancer
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.

Nastorazepide Z-360	Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt	Neurological Disease Cancer
Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [ ³H]CCK-8 to the human CCK-2 receptor with a K_i value of 0.47 nM. Nastorazepide inhibits *IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt* and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain ^[1] .

Nastorazepide hemicalcium Z-360 hemicalcium	Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt	Neurological Disease Cancer
Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [ ³H]CCK-8 to the human CCK-2 receptor with a K_i value of 0.47 nM. Nastorazepide hemicalcium inhibits *IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt* and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain ^[1] .

Nastorazepide (Standard)	Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt	Neurological Disease Cancer
Nastorazepide (Standard) is the analytical standard of Nastorazepide. This product is intended for research and analytical applications. Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain ^[1] .

GN44028 5 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC₅₀ of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers ^[1] .

Oltipraz 20+ Cited Publications RP 35972; NSC 347901	HIF/HIF Prolyl-Hydroxylase HIV Keap1-Nrf2 Parasite	Cancer
Oltipraz has an inhibitory effect on *HIF-1α* activation in a time-dependent manner, completely abrogating *HIF-1α* induction at ≥10 μM concentrations, the IC₅₀ of Oltipraz for *HIF-1α* inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.

Oltipraz-d3 RP 35972-d₃; NSC 347901-d₃	Isotope-Labeled Compounds HIF/HIF Prolyl-Hydroxylase HIV Keap1-Nrf2	Cancer
Oltipraz-d₃ is the deuterium labeled Oltipraz. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.

Oltipraz (Standard)	HIF/HIF Prolyl-Hydroxylase HIV Keap1-Nrf2 Parasite	Cancer
Oltipraz (Standard) is the analytical standard of Oltipraz. This product is intended for research and analytical applications. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.

O-Carboranylphenoxyacetanilide	HIF/HIF Prolyl-Hydroxylase HSP	Cancer
O-Carboranylphenoxyacetanilide is a *HIF-1α* inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC₅₀: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity ^[1].

HIF-IN-1	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF)-1 inhibitor. HIF-IN-1 suppresses HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA. HIF-IN-1 shows no obvious cytotoxicity ^[1].

CTK7A	Epigenetic Reader Domain Histone Acetyltransferase HIF/HIF Prolyl-Hydroxylase	Cancer
CTK7A is a curcumin derivative with anticancer activity by inhibiting the HAT activity of p300 and reducing the autoacetylation of p300, thereby affecting its interaction with *HIF-1α. The inhibition of CTK7A leads to decreased HIF-1α* accumulation and activity, which can be used for cancer treatment research ^[1].

Fraxinellone 4 Publications Verification	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT	Inflammation/Immunology Cancer
Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a *PD-L1* inhibitor and inhibits *HIF-1α* protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 ^[1].

VHL-IN-1	Ligands for E3 Ligase HIF/HIF Prolyl-Hydroxylase	Cancer
VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs) ^[1].

Cyclo(CRVIIF)	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CRVIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 65 and 123 μM, respectively ^[1].

Dimethyl-bisphenol A DMBPA	HIF/HIF Prolyl-Hydroxylase	Cancer
Dimethyl-bisphenol A (DMBPA) is a potent *HIF-1α* inhibitor. Dimethyl-bisphenol A can decrease Vegfa mRNA expression ^[1].

Cyclo(CKLIIF) TFA	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CKLIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 2.6 and 2.2 μM, respectively ^[1].

Cyclo(CRLLIF)	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 14.5 and 10.2 μM, respectively ^[1].

KCN1	HIF/HIF Prolyl-Hydroxylase Histone Acetyltransferase	Cancer
KCN1 is a *p300/HIF-1α* interaction inhibitor. KCN1 inhibits HIF transcriptional activity by binding to the CH1 domain of p300 and preventing the p300/HIF-1α assembly. KCN1 exerts antitumor activities through cell cycle arrest ^[1] .

GEM-5	HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53	Cancer
GEM-5 is a gemcitabine-based conjugate containing a *HIF-1α* inhibitor (YC-1) (IC₅₀=30 nM). GEM-5 can significantly down-regulate the expression of *HIF-1α* and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth ^[1].

Fraxinellone (Standard)	Reference Standards PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT	Inflammation/Immunology Cancer
Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 ^[1].

FM19G11	HIF/HIF Prolyl-Hydroxylase	Neurological Disease Cancer
FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC₅₀ of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions ^[1] .

EZN-2968 RO 707179	HIF/HIF Prolyl-Hydroxylase	Cancer
EZN-2968 is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968, inhibits tumor cell growth.

EZN-2968 sodium	HIF/HIF Prolyl-Hydroxylase	Cancer
EZN-2968 sodium is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968 sodium, inhibits tumor cell growth.

7-Hydroxyneolamellarin A	HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer ^[1].

LW1564	HIF/HIF Prolyl-Hydroxylase AMPK	Cancer
LW1564 is an inhibitor for *HIF-1α* with an IC₅₀ of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI₅₀ of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model ^[1].

PX-478 75+ Cited Publications	HIF/HIF Prolyl-Hydroxylase Autophagy	Cancer
PX-478 is an orally active *HIF-1α* inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier ^[1] .

AFP464 dihydrochloride NSC710464 dihydrochloride	HIF/HIF Prolyl-Hydroxylase	Cancer
AFP464 (dihydrochloride) (NSC710464 (dihydrochloride)) is the hydrochloride form of AFP464 and is a potent *HIF-1α* inhibitor with an IC₅₀ value of 0.25 μM. It is also an activator of aryl hydrocarbon receptor (AhR).

AJM 290	HIF/HIF Prolyl-Hydroxylase	Cancer
AJM 290 is a *Trx-1* inhibitor. AJM 290 is an inhibitor of the HIF-1α COOH-terminal transactivation domain, and blocks HIF-1 binding to DNA ^[1].

AFP464 free base NSC710464 free base	HIF/HIF Prolyl-Hydroxylase	Cancer
AFP464 free base (NSC710464 free base), is an active *HIF-1α* inhibitor with an IC₅₀ of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.

DMOG Dimethyloxallyl Glycine	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
DMOG (GMP) is the GMP level of DMOG (HY-15893). 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) ^[1].

Panaxadiol 3 Publications Verification 20(R)-Panaxadiol	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT	Cancer
Panaxadiol (20(R)-Panaxadiol) is an orally active *HIF-1α/STAT3* inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities ^[1] .

Velutin	HIF/HIF Prolyl-Hydroxylase	Inflammation/Immunology
Velutin is an aglycone extracted from Flammulina velutipes, with inhibitory activity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway ^[1] .

Cat. No.	Product Name

HY-L045

Oxygen Sensing Compound Library

3,434 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 3,434 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-100575

Acriflavine

5+ Cited Publications

Acriflavinium chloride 3,6-Acridinediamine mix

Fluorescent Dyes/Probes

Acriflavine (Acriflavinium chloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine is an antiseptic agent. Acriflavine is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2 ^[1] .

HY-D2360

O-Carboranylphenoxyacetanilide	Fluorescent Dyes/Probes
O-Carboranylphenoxyacetanilide is a *HIF-1α* inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC₅₀: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity ^[1].

HY-15893G

DMOG (GMP)

Dimethyloxallyl Glycine (GMP)

Fluorescent Dye

DMOG (GMP) is the GMP level of DMOG (HY-15893). 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) ^[1].

HY-12519G

Oltipraz (GMP) RP 35972 (GMP); NSC 347901 (GMP)	Fluorescent Dye
Oltipraz (GMP) is Oltipraz (HY-12519) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Oltipraz has an inhibitory effect on HIF-1α activation. Oltipraz is a potent Nrf2 activator ^[1] .

Cat. No.	Product Name	Type

HY-15893G

DMOG (GMP)

Dimethyloxallyl Glycine (GMP)

Biochemical Assay Reagents

HY-12519G

Oltipraz (GMP) RP 35972 (GMP); NSC 347901 (GMP)	Biochemical Assay Reagents
Oltipraz (GMP) is Oltipraz (HY-12519) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Oltipraz has an inhibitory effect on HIF-1α activation. Oltipraz is a potent Nrf2 activator ^[1] .

Cat. No.	Product Name	Target	Research Area

HY-P1888

HIF-1 alpha (556-574)	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
HIF-1 alpha (556-574) is a short hypoxia-inducible factor-1 (HIF-1) 19 residues fragment. HIF-1 functions as master regulator of response to oxygen homeostasis ^[1].

HY-P10221A

Cyclo(CKLIIF) TFA	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CKLIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 2.6 and 2.2 μM, respectively ^[1].

HY-P5908F

FAM-DEALA-Hyp-YIPD	Peptides	Others
FAM-DEALA-Hyp-YIPD is a fluorescent *HIF-1α* peptide, with the K_d of 180-560 nM. FAM-DEALA-Hyp-YIPD can be used to assess VHL binding in Fluorescence Polarization (FP) displacement assay, and evaluate the effect of VHL binding on degradation activity ^[1].

HY-P2324

Gramicidin A 1 Publications Verification	Bacterial HIF/HIF Prolyl-Hydroxylase Antibiotic	Infection Cancer
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α) ^[1] .

HY-P1888A

HIF-1 alpha (556-574) TFA	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease
HIF-1 alpha (556-574) TFA is a short hypoxia-inducible factor-1 (HIF-1) 19 residues fragment. HIF-1 functions as master regulator of response to oxygen homeostasis ^[1].

HY-P5908

DEALA-Hyp-YIPD	Peptides	Cardiovascular Disease
DEALA-Hyp-YIPD is an HIF-1α peptide that inhibits VHL/HIF-1α interaction with an IC₅₀ of 0.91 μM and a K_d of 180 nM ^[1].

HY-P10223

Cyclo(CRVIIF)	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CRVIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 65 and 123 μM, respectively ^[1].

HY-P10222

Cyclo(CRLLIF)	HIF/HIF Prolyl-Hydroxylase	Cancer
Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains K_D of 14.5 and 10.2 μM, respectively ^[1].

HY-P5915

FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2	HIF/HIF Prolyl-Hydroxylase	Cancer
FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2, a 5-FAM labeled HIF-1α peptide, is a substrate of VHL. FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2 binds to VHL protein with a K_D of 3 nM. Ex/Em (λ) = 485/520 nm ^[1].

HY-P2324A

Gramicidin A TFA	Antibiotic Bacterial	Infection
Gramicidin A (TFA) is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A (TFA) is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A (TFA) induces degradation of hypoxia inducible factor 1 α (HIF-1α) ^[1] .

HY-P10426

cyclo(CLLFVY)	HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC₅₀ of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers ^[1].

HY-P2657

Verucopeptin	HIF/HIF Prolyl-Hydroxylase Proton Pump Endogenous Metabolite	Cancer
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.

HY-P1420

TAT-cyclo-CLLFVY 2 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of *HIF-1* heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts *HIF-1α/HIF-1β* protein-protein interaction with an IC₅₀ of 1.3 μM ^[1].

HY-P1420A

TAT-cyclo-CLLFVY TFA	HIF/HIF Prolyl-Hydroxylase	Cancer
TAT-cyclo-CLLFVY TFA is a cyclic peptide inhibitor of *HIF-1* heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY TFA disrupts *HIF-1α/HIF-1β* protein-protein interaction with an IC₅₀ of 1.3 μM ^[1].

HY-P10797

TAT-N24	NF-κB HIF/HIF Prolyl-Hydroxylase VEGFR TNF Receptor Interleukin Related	Cardiovascular Disease Inflammation/Immunology
TAT-N24 is a cell-permeable TAT peptide as a p55PIK signaling inhibitor. TAT-N24 is effective for corneal neovascularization (CNV) and ocular inflammation by inhibiting the *HIF-1α/NF-κB* signaling pathway in corneal suture (CS). TAT-N24 also inhibits corneal neovascularization ^[1].

HY-P10869

dCNP 1 Publications Verification	Natriuretic Peptide Receptor (NPR)	Inflammation/Immunology Cancer
dCNP binds to NPR-B/C receptor, activates cGMP signaling pathway, and regulates vascular function. dCNP exhibits anti-hypoxia property through downregulation of hypoxia-related genes expressions like HIF1α and HIF2α. dCNP inhibits the induction of tumor stroma and exhibits anti-fibrosis activity. dCNP upregulates CTLs, NK cells, and conventional type 1 dendritic cells in tumors, and activates immune responses ^[1].

Cat. No.	Product Name	Target	Research Area

HY-P991664

AG01	Src Akt ERK TAM Receptor c-Met/HGFR MMP HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, *HIF-1α, and VEGF*. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers ^[1].

Cat. No.	Compare	Product Name	Species	Source

HY-P74888

	HIF-1 alpha Protein, Human (His) 3 Publications Verification Hypoxia-inducible factor 1-alpha; HIF-1-alpha; BHLHE78; HIF1A; MOP1; PASD8	Human	E. coli
	HIF-1 alpha is a key protein that responds to low oxygen levels. HIF-1 alpha Protein, Human (His) is the recombinant human-derived HIF-1 alpha protein, expressed by E. coli , with N-His labeled tag.

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HY-P84619

	HIF1 alpha Antibody (YA4316) HIF1; MOP1; PASD8; bHLHe78; HIF-1alpha; HIF1-ALPHA; HIF1A	WB, IHC-P, ICC/IF, ELISA	Human, Mouse, Monkey
	HIF1 alpha Antibody (YA4316) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to HIF1 alpha.

HY-P85711

	HIF1 alpha Antibody (YA5403) Hypoxia-inducible factor 1-alpha; HIF-1-alpha; HIF1-alpha; ARNT-interacting protein; Basic-helix-loop-helix-PAS protein MOP1; Class E basic helix-loop-helix protein 78; bHLHe78; Member of PAS protein 1; PAS domain-containing protein 8;	IHC-P, WB	Human, Mouse, Rat
	HIF1 alpha Antibody (YA5403) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to HIF1 alpha.

HY-P80704

	HIF1 alpha Antibody 5 Publications Verification HIF1A; BHLHE78; MOP1; PASD8; Hypoxia-inducible factor 1-alpha; HIF-1-alpha; HIF1-alpha; ARNT-interacting protein; Basic-helix-loop-helix-PAS protein MOP1; Class E basic helix-loop-helix protein 78; bHLHe78; Member of PAS protein 1; PAS doma	ICC/IF, WB, IHC-F, IHC-P, ELISA	Human, Mouse, Rat
	HIF1 alpha Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to HIF1 alpha.

HY-P81153

	*HIF-2 alpha* Antibody (YA3517)** Basic helix loop helix PAS protein MOP2; Basic-helix-loop-helix-PAS protein MOP2; bHLHe73; Class E basic helix-loop-helix protein 73; ECYT4; Endothelial PAS domain containing protein 1; Endothelial pas domain protein 1; Endothelial PAS domain-containing protein 1; EPAS 1; EPAS-1; EPAS1; EPAS1_HUMAN; HIF 1 alpha like factor; HIF-1-alpha-like factor; HIF-2-alpha; HIF2-alpha; HIF2A; HLF; Hypoxia inducible factor 2 alpha; Hypoxia inducible factor 2 alpha subunit; Hypoxia-inducible factor 2-alpha; Member of PAS protein 2; Member of pas superfamily 2; MOP 2; MOP2; PAS domain-containing protein 2; PASD2.	WB, IHC-P, FC	Human, Mouse, Rat
	HIF-2 alpha Antibody (YA3517) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to HIF-2 alpha.

HY-P85201

	HIF1 alpha Antibody (YA4893) HIF1A; BHLHE78; MOP1; PASD8; Hypoxia-inducible factor 1-alpha; HIF-1-alpha; HIF1-alpha; ARNT-interacting protein; Basic-helix-loop-helix-PAS protein MOP1; Class E basic helix-loop-helix protein 78; bHLHe78; Member of PAS protein 1; PAS doma	WB, IHC-P, ICC/IF, ELISA	Human, Mouse, Monkey
	HIF1 alpha Antibody (YA4893) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to HIF1 alpha.

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HY-N0171

Beta-Sitosterol (purity>80%) 10+ Cited Publications		Cholesterol
Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, *TNF-α, IL-1β, and NF-κB p65* and restoring the activity of the *HIF-1α/mTOR* signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc ^[1] .

HY-158826

EZN-2968 RO 707179		Antisense Oligonucleotides
EZN-2968 is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968, inhibits tumor cell growth.

HY-158826A

EZN-2968 sodium		Antisense Oligonucleotides
EZN-2968 sodium is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968 sodium, inhibits tumor cell growth.

HY-RS16959

Hif1a Mouse Pre-designed siRNA Set A		siRNAs Mouse Pre-designed siRNA Sets
Hif1a Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hif1a gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

HY-RS06168

HIF1A Human Pre-designed siRNA Set A		siRNAs Human Pre-designed siRNA Sets
HIF1A Human Pre-designed siRNA Set A contains three designed siRNAs for HIF1A gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

HY-RS23402

Hif1a Rat Pre-designed siRNA Set A		siRNAs Rat Pre-designed siRNA Sets
Hif1a Rat Pre-designed siRNA Set A contains three designed siRNAs for Hif1a gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

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