Search Result

Results for "

HIF-α1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	HIF/HIF Prolyl-Hydroxylase (60) ADC Cytotoxin (2) Akt (6) Amyloid-β (1) Antibiotic (14) AP-1 (1) Apoptosis (15) ATP Synthase (1) Autophagy (7) Bacterial (8) Beclin1 (2) Calcium Channel (3) Cholinesterase (ChE) (1) DNA/RNA Synthesis (1) Endogenous Metabolite (2) Fungal (3) HIV (2) HSP (1) Influenza Virus (2) Isotope-Labeled Compounds (3) JNK (2) Keap1-Nrf2 (3) Ligands for E3 Ligase (1) MDM-2/p53 (6) MicroRNA (3) Microtubule/Tubulin (4) Mitochondrial Metabolism (1) MMP (2) Monoamine Oxidase (1) mTOR (3) NF-κB (2) Oxidative Phosphorylation (2) Parasite (4) PD-1/PD-L1 (2) PI3K (1) Potassium Channel (3) PPAR (1) PROTACs (1) Proton Pump (1) Ras (1) Reactive Oxygen Species (4) STAT (3) Topoisomerase (2) VEGFR (5) Xanthine Oxidase (2)
By Research Areas:	Cancer (61) Cardiovascular Disease (7) Infection (17) Inflammation/Immunology (13) Metabolic Disease (8) Neurological Disease (11)

By Targets:

HIF/HIF Prolyl-Hydroxylase (60)

ADC Cytotoxin (2)

Akt (6)

Amyloid-β (1)

Antibiotic (14)

AP-1 (1)

Apoptosis (15)

ATP Synthase (1)

Autophagy (7)

Bacterial (8)

Beclin1 (2)

Calcium Channel (3)

Cholinesterase (ChE) (1)

DNA/RNA Synthesis (1)

Endogenous Metabolite (2)

Fungal (3)

HIV (2)

HSP (1)

Influenza Virus (2)

Isotope-Labeled Compounds (3)

JNK (2)

Keap1-Nrf2 (3)

Ligands for E3 Ligase (1)

MDM-2/p53 (6)

MicroRNA (3)

Microtubule/Tubulin (4)

Mitochondrial Metabolism (1)

MMP (2)

Monoamine Oxidase (1)

mTOR (3)

NF-κB (2)

Oxidative Phosphorylation (2)

Parasite (4)

PD-1/PD-L1 (2)

PI3K (1)

Potassium Channel (3)

PPAR (1)

PROTACs (1)

Proton Pump (1)

Ras (1)

Reactive Oxygen Species (4)

STAT (3)

Topoisomerase (2)

VEGFR (5)

Xanthine Oxidase (2)

By Research Areas:

Cancer (61)

Cardiovascular Disease (7)

Infection (17)

Inflammation/Immunology (13)

Metabolic Disease (8)

Neurological Disease (11)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: HIF/HIF Prolyl-Hydroxylase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111387

IDF-11774

4 Publications Verification

HIF/HIF Prolyl-Hydroxylase Cancer

IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC₅₀ of 3.65 μM.

IDF-11774 4 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC₅₀ of 3.65 μM.

HY-B0639

Amifostine 5 Publications Verification WR2721	MDM-2/p53 HIF/HIF Prolyl-Hydroxylase	Cancer
Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action .

HY-B0639A

Amifostine trihydrate 5 Publications Verification WR2721 trihydrate	MDM-2/p53 HIF/HIF Prolyl-Hydroxylase	Cancer
Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine trihydrate protects cells from damage by scavenging oxygen-derived free radicals. Amifostine trihydrate reduces renal toxicity and has antiangiogenic action .

HY-110266

GN44028 4 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 .

HY-13671

LW6 15+ 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 of 4.4 μM. LW6 decreases *HIF-1α* protein expression without affecting HIF-1β expression.

HY-149635

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 .

HY-12519

Oltipraz 10+ 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.

HY-146144

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 .

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 .

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 .

HY-P10221

Cyclo(CKLIIF)	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 .

HY-12519S

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.

HY-151344

HIF-1/2α-IN-2	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1/2α-IN-2 is an inhibitor of *HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α* levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2) .

HY-115903A

HIF-1α-IN-2 hydrochloride	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 .

HY-115903

HIF-1α-IN-2	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 .

HY-153017

HIF-1 inhibitor-4	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1 inhibitor-4 is a *HIF-1* inhibitor (IC₅₀: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level .

HY-147813

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 .

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 .

HY-163370

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 .

HY-N10330

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 .

HY-N0242

Fraxinellone 1 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 .

HY-156106

VHL-IN-1	PROTACs 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) .

HY-151465

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 .

HY-15672

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 .

HY-18371

TC-S 7009	HIF/HIF Prolyl-Hydroxylase	Inflammation/Immunology
TC-S 7009 is a potent and selective *HIF-2α* inhibitor with a K_d of 81 nM. TC-S 7009 is more selective for *HIF-2α* than HIF-1α (K_d ≫ 5 μM). TC-S 7009 disrupts *HIF-2α* heterodimerization, decreases DNA-binding activity, and reduces *HIF-2α* target gene expression .

HY-151466

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 .

HY-151341

HIF-1/2α-IN-1	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1/2α-IN-1 is an orally active *HIF-2α* inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC₅₀ value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) .

HY-115746

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 .

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 .

HY-146540

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 .

HY-10231

PX-478 30+ 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 .

HY-17412S

Minocycline-d6 hydrochloride	Isotope-Labeled Compounds Antibiotic	Others
Minocycline-d₆ hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and *HIF-1α* inhibitor .

HY-16031B

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).

HY-16031

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.

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) .

HY-15893

DMOG Dimethyloxallyl Glycine	HIF/HIF Prolyl-Hydroxylase Autophagy	Cancer
DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of *HIF-PH, which results in HIF-1α* stabilisation and accmulation in vitro and in vivo . DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal . DMOG induces cell autophagy .

HY-B0219

Allopurinol 4 Publications Verification	Xanthine Oxidase	Infection Neurological Disease Inflammation/Immunology Cancer
Allopurinol is a potent and orally active xanthine oxidase inhibitor with an IC₅₀ value of 0.2-50 μM. Allopurinol can be used in the research of hyperuricemia and gout. Allopurinol decreases the expression of HIF-1α and HIF-2α protein. Allopurinol shows anti-depressant and anti-nociception activity. Anti-leishmanial effect .

HY-N0596

Panaxadiol 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 .

HY-B0219A

Allopurinol sodium 4 Publications Verification	Xanthine Oxidase	Infection Neurological Disease Inflammation/Immunology Cancer
Allopurinol sodium is a potent and orally active xanthine oxidase inhibitor with an IC₅₀ value of 0.2-50 μM. Allopurinol sodium can be used in the research of hyperuricemia and gout. Allopurinol sodium decreases the expression of HIF-1α and HIF-2α protein. Allopurinol sodium shows anti-depressant and anti-nociception activity. Anti-leishmanial effect .

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-N1098

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 .

HY-N6782

Oligomycin 25+ 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 .

HY-122094

Steppogenin	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease Cancer
Steppogenin is a potent inhibitor of *HIF-1α* and DLL4, with IC₅₀ values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors .

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) .

HY-119264A

PRLX-93936 dihydrochloride	HIF/HIF Prolyl-Hydroxylase Ras	Cancer
PRLX-93936 dihydrochloride (Compound 16) is a *HIF-1α* inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma .

HY-120087

KG-548	HIF/HIF Prolyl-Hydroxylase	Cancer
KG-548 is an ARNT/TACC3 disruptor and a *HIF-1α* inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as *HIF-β* .

HY-142693

Angiogenesis agent 1	HIF/HIF Prolyl-Hydroxylase	Metabolic Disease
Angiogenesis agent 1 (compound C-31) is a salidroside-derivated glycoside analogue. Angiogenesis agent 1 is an activator of the HIF-1α pathway. Angiogenesis agent 1 has the potential for the research of diabetic hind limb ischemia .

HY-N2187

Deoxyshikonin 1 Publications Verification
Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF. Deoxyshikonin inhibited colorectal cancer (CRC) through the PI3K/Akt/mTOR pathway. Deoxyshikonin has proangiogenesis effect and antitumor activity. Deoxyshikonin is an antibacterial agent against methicillin-resistant S. aureus (MRSA) and S. pneumonia (MIC=17 μg/mL) .

HY-16560

Camptothecin 35+ Cited Publications Campathecin; (S)-(+)-Camptothecin; CPT	Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic	Infection Cancer
Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC₅₀ of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .

HY-B0413S

Fenbendazole-d3 2 Publications Verification	HIF/HIF Prolyl-Hydroxylase Parasite Microtubule/Tubulin Antibiotic	Infection
Fenbendazole-d₃ is a deuterium labeled Fenbendazole. Fenbendazole-d₃ is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1][2][3][4].

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 .

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 .

Cat. No.	Product Name

HY-L045

Oxygen Sensing Compound Library

2507 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 2507 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-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) .

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 .

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 .

HY-P10221

Cyclo(CKLIIF)	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 .

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 .

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-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) .

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 .

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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0242

Fraxinellone 1 Publications Verification	Classification of Application Fields Terpenoids Dictamnus dasycarpus Turcz. Sesquiterpenes Source classification Rutaceae Plants Inflammation/Immunology Disease Research Fields	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT
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 .

HY-N0596

Panaxadiol 20(R)-Panaxadiol	Panax ginseng C. A. Meyer Triterpenes Structural Classification Classification of Application Fields Terpenoids Source classification Plants Disease Research Fields Araliaceae Cancer	PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT
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 .

HY-N1098

Velutin	Flavonoids other families Microorganisms Classification of Application Fields Flavones Source classification Phenols Polyphenols Plants Inflammation/Immunology Disease Research Fields	HIF/HIF Prolyl-Hydroxylase
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 .

HY-N6782

Oligomycin 25+ Cited Publications	Infection Structural Classification Microorganisms Antifungal Macrolide Antibiotics Classification of Application Fields Antibiotics Source classification Disease Research Anticancer Disease Research Fields	Oxidative Phosphorylation ATP Synthase Fungal Antibiotic
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 .

HY-N10330

7-Hydroxyneolamellarin A	Structural Classification Animals Source classification Phenols	HIF/HIF Prolyl-Hydroxylase VEGFR
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 .

HY-122094

Steppogenin	Structural Classification Flavonoids Flavones Source classification Maclura tricuspidata Carriere Plants Moraceae	HIF/HIF Prolyl-Hydroxylase
Steppogenin is a potent inhibitor of *HIF-1α* and DLL4, with IC₅₀ values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors .

HY-16560

Camptothecin Maximum Cited Publications 38 Publications Verification Campathecin; (S)-(+)-Camptothecin; CPT	Infection Alkaloids Structural Classification Classification of Application Fields Source classification Quinoline Alkaloids Camptotheca acuminata Decne. Plants Nyssaceae Disease Research Fields	Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic
Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC₅₀ of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .

HY-N5136

25(R,S)-Ruscogenin	Liliaceae Microorganisms Classification of Application Fields Source classification Liriope platyphylla Wang et Tang Plants Disease Research Fields Steroids Cancer	Apoptosis PI3K Akt mTOR
Ruscogenin suppresses HCC metastasis by reducing the expression of MMP-2, MMP-9, uPA, VEGF and HIF-1α via regulating the PI3K/Akt/mTOR signaling pathway . And Ruscogenin alleviates LPS-induced pulmonary endothelial cell apoptosis by su

HY-N5112B

β,β-Dimethylacrylshikonin 1 Publications Verification Isoarnebin I	Quinones Structural Classification Classification of Application Fields Source classification Phenols Polyphenols Plants Lithospermum erythrorhizon Sieb. et Zucc. Naphthalene Quinones Disease Research Fields Boraginaceae Cancer	HIF/HIF Prolyl-Hydroxylase
β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative isolated from Lithospermum erythrorhizon Sieb. et Zucc. , promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway.β,β-Dimethylacrylshikonin has anti-tumor activity .

HY-N2425

Rhodiosin	Flavonols Structural Classification Classification of Application Fields Source classification Crassulaceae Metabolic Disease Plants Rhodiola crenulata (HK. f. et.Thoms) H. Ohba Flavonoids Rhodiola rosea Linn. Phenols Polyphenols Disease Research Fields	Cholinesterase (ChE)
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC₅₀ for CYP2D6 is 0.761 μM, and the K_i is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system

HY-B0239

Chloramphenicol 5+ Cited Publications	Structural Classification Classification of Application Fields Anti-aging Source classification Antibacterial Disease Research Endogenous metabolite Other Antibiotics Infection Human Gut Microbiota Metabolites Plant Cell Culture Microorganisms Antibiotics Resistance Selection Animal Husbandry Anticancer Disease Research Fields Cancer	Antibiotic Bacterial HIF/HIF Prolyl-Hydroxylase VEGFR Autophagy Apoptosis Beclin1 JNK Akt MMP
Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .

HY-N0234

Bavachinin 2 Publications Verification 7-O-Methylbavachin; Bavachinin A	Structural Classification Monophenols Flavonoids Classification of Application Fields Leguminosae Flavonones Source classification Phenols Psoralea corylifolia L. Plants Inflammation/Immunology Disease Research Fields	Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase
Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC₅₀ value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of *HIF-1α*. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .

HY-N0787

Cryptochlorogenic acid 1 Publications Verification 4-Caffeoylquinic acid; 4-O-Caffeoylquinic acid	Structural Classification Classification of Application Fields Source classification Plants Moraceae Endogenous metabolite Simple Phenylpropanols Other Diseases Phenols Polyphenols Phenylpropanoids Disease Research Fields Morus alba Linn.	Endogenous Metabolite NF-κB Keap1-Nrf2 mTOR HIF/HIF Prolyl-Hydroxylase
Cryptochlorogenic acid (4-Caffeoylquinic acid) is a naturally occurring phenolic acid compound with oral effectiveness, anti-inflammatory, antioxidant and anti-cardiac hypertrophy effects. Alleviating LPS (HY-D1056) and ISO (HY-B0468) by regulating proinflammatory factor expression, inhibiting NF-κB activity, promoting Nrf2 nuclear transfer, and regulating PI3Kα/Akt/ mTOR / *HIF-1α* signaling pathway Induced physiological stress response .

Cat. No.	Product Name	Chemical Structure

HY-B0413S

Fenbendazole-d3

2 Publications Verification

Fenbendazole-d₃ is a deuterium labeled Fenbendazole. Fenbendazole-d₃ is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1][2][3][4].

HY-17412S1

Minocycline-d6 sulfate
Minocycline-d₆ sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.

HY-16560S

Camptothecin-d5

Camptothecin-d₅ is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].

HY-12519S

Oltipraz-d3
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.

HY-17412S

Minocycline-d6 hydrochloride
Minocycline-d₆ hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and *HIF-1α* inhibitor .

HY-B0239S2

Threo-Chloramphenicol-d6

Threo-Chloramphenicol-d₆ is the deuterium labeled Chloramphenicol[1]. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research[2][3][4].

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