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HIF Activator

" in MedChemExpress (MCE) Product Catalog:

32

Inhibitors & Agonists

2

Fluorescent Dye

1

Biochemical Assay Reagents

1

Peptides

7

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2

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12519
    Oltipraz
    Maximum Cited Publications
    17 Publications Verification

    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
  • HY-12754
    ML228
    5+ Cited Publications

    CID-46742353

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF .
    ML228
  • 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).
    AFP464 dihydrochloride
  • HY-123422
    GSK360A

    		HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) .
    GSK360A
  • HY-29090
    ML228 analog

    		HIF/HIF Prolyl-Hydroxylase Cancer
    ML228 analog is an analog of ML228 (HY-12754). ML228 is a potent activator of HIF .
    ML228 analog
  • 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.
    Oltipraz-d3
  • HY-D2360
    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 .
    O-Carboranylphenoxyacetanilide
  • HY-18259
    103D5R

    		HIF/HIF Prolyl-Hydroxylase Cancer
    103D5R (Compound 15) is an inhibitor for the activation of hypoxia-inducible factor-1 (HIF-1) with an IC50 of 35 µM, through reduction of the HIF-1α protein synthesis. 103D5R inhibits the proliferation of LN229 with IC50 of 26 µM .
    103D5R
  • HY-12519G
    Oltipraz (GMP)

    RP 35972 (GMP); NSC 347901 (GMP)

    		 HIF/HIF Prolyl-Hydroxylase HIV Keap1-Nrf2 Parasite Cancer
    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 .
    Oltipraz (GMP)
  • 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.
    AFP464 free base
  • HY-119264
    PRLX-93936

    		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 .
    PRLX-93936
  • 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 .
    PRLX-93936 dihydrochloride
  • 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 .
    Angiogenesis agent 1
  • HY-170027
    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 .
    LW1564
  • HY-B0413S
    Fenbendazole-d3
    3 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].
    Fenbendazole-d3
  • HY-111431
    p-Cresyl sulfate
    5 Publications Verification

    p-Tolyl sulfate

    		 JNK p38 MAPK Reactive Oxygen Species Metabolic Disease
    p-Cresyl sulfate (p-Tolyl sulfate) is a uremic toxin, that can cause renal damage and dysfunction. p-Cresyl sulfate shows antiproliferation activity. p-Cresyl sulfate increases the protein expression of HIF-1α and VHL, decreases the protein expression of HIF-2α. p-Cresyl sulfate induces epithelial-mesenchymal transition (EMT). p-Cresyl sulfate activates the JNK and p38 MAPK signaling pathways .
    p-Cresyl sulfate
  • HY-P10869
    dCNP

    		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 .
    dCNP
  • HY-161838
    ICT10336

    		ATM/ATR Cancer
    ICT10336 is a hypoxia-responsive prodrug of ATR inhibitor, AZD6738 (HY-19323). ICT10336 is hypoxia-activated and specifically releases AZD6738 only in hypoxic conditions in vitro. This can inhibit ATR activation (T1989 and S428 phosphorylation) and subsequently abrogate HIF1a-mediated adaptation of hypoxic cancers cells, thus selectively inducing cell death in 2D and 3D cancer models. ICT10336 is a metabolic substrate of CYPOR activity.
    ICT10336
  • HY-B0413
    Fenbendazole
    5 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 .
    Fenbendazole
  • HY-N3005
    Britannin
    1 Publications Verification

    		 Apoptosis Autophagy NOD-like Receptor (NLR) Pyroptosis Inflammation/Immunology Cancer
    Britannin is an NLRP3 inhibitor with an IC50 of 3.630 μM, exhibiting anti-inflammatory activity. Britannin inhibits the activation and assembly of the NLRP3 inflammasome by blocking the interaction between NLRP3 and NEK7. Additionally, Britannin demonstrates antitumor activity by inhibiting the proliferation of tumor cells through blocking the interaction between HIF-1α and Myc, thereby suppressing PD-L1 expression and enhancing cytotoxic T lymphocyte activity. Britannin can also induce apoptosis and autophagy in liver cancer cells by activating ROS-regulated AMPK. Britannin holds promise for research in the fields of anti-inflammatory and antitumor therapeutics .
    Britannin
  • HY-N0234
    Bavachinin
    3 Publications Verification

    7-O-Methylbavachin; Bavachinin A

    		 Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Cancer
    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. .
    Bavachinin
  • HY-B0413R
    Fenbendazole (Standard)

    		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 .
    Fenbendazole (Standard)
  • HY-110294
    CM037

    A37

    		 Aldehyde Dehydrogenase (ALDH) Cancer
    CM037 is a highly selective and competitive ALDH1A1 inhibitor (IC50=4.6 μM). CM037 blocks the catalytic activity of ALDH1A1, thereby inhibiting the activation of the downstream HIF-1α/VEGF pathway. CM037 is mainly used to study the ALDH1A1-mediated regulation of cancer stem cells (CSCs) and angiogenesis, especially in breast cancer, showing the potential to inhibit tumor angiogenesis and stem cell characteristics .
    CM037
  • HY-148877
    AT-533

    		HSP HSV HIF/HIF Prolyl-Hydroxylase VEGFR NF-κB ERK Akt FAK Infection Inflammation/Immunology Cancer
    AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs) .
    AT-533
  • HY-N5112B
    β,β-Dimethylacrylshikonin
    1 Publications Verification

    Isoarnebin I

    		 HIF/HIF Prolyl-Hydroxylase Apoptosis Notch NO Synthase Bcl-2 Family Cancer
    β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative that can be isolated from Lithospermum erythrorhizon Sieb. et Zucc. β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin inhibits Notch-1 activation. β,β-Dimethylacrylshikonin inhibtis tumor cell proliferation, induces tumor cell apoptosis, and inhibits tumor growth .
    β,β-Dimethylacrylshikonin
  • HY-W016409
    Ethyl 3,4-dihydroxybenzoate
    1 Publications Verification

    Protocatechuic acid ethyl ester

    		 HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species NO Synthase Autophagy Apoptosis Metabolic Disease Cancer
    Ethyl 3,4-dihydroxybenzoate (EDHB) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema .
    Ethyl 3,4-dihydroxybenzoate
  • HY-N0234R
    Bavachinin (Standard)

    		Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. 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. .
    Bavachinin (Standard)
  • HY-128872
    Etrinabdione

    EHP-101; VCE-​004.8

    		 PPAR Cannabinoid Receptor HIF/HIF Prolyl-Hydroxylase Metabolic Disease Inflammation/Immunology
    Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity .
    Etrinabdione
  • HY-B1080
    Tilorone dihydrochloride
    2 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Influenza Virus Infection Neurological Disease
    Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS .Tilorone dihydrochloride exhibits an inhibitory activity with EC50 of 230 nM against Ebola virus (EBOV) .
    Tilorone dihydrochloride
  • HY-B1080R
    Tilorone (dihydrochloride) (Standard)

    		HIF/HIF Prolyl-Hydroxylase Influenza Virus Infection Neurological Disease
    Tilorone (dihydrochloride) (Standard) is the analytical standard of Tilorone (dihydrochloride). This product is intended for research and analytical applications. Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS .Tilorone dihydrochloride exhibits an inhibitory activity with EC50 of 230 nM against Ebola virus (EBOV) .
    Tilorone (dihydrochloride) (Standard)
  • HY-120793
    CMC2.24

    TRB-N0224

    		 Ras Apoptosis MMP Inflammation/Immunology Cancer
    CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis .
    CMC2.24
  • HY-130413
    Protectin D1

    Neuroprotectin D1; NPD1

    		 Endogenous Metabolite PI3K Akt HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species Caspase Interleukin Related MicroRNA Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Protectin D1, a neuroprotectin D1 produced by neuronal cells, is a member of a newly discovered family of bioactive products derived from docosahexaenoic acid. Protectin D1 also serves as a specialized pro-resolving mediator, exhibiting effective in vivo pro-resolving activity in various human disease models. Additionally, Protectin D1 is an inhibitor of NALP3 inflammasomes and regulates the PI3K/AKT and HIF-1α signaling pathways. Protectin D1 exerts anti-inflammatory effects by reducing ROS levels, inhibiting the expression of NALP3, ASC, and Caspase-1, and consequently decreasing the release of pro-inflammatory cytokines IL-1β and IL-18. Furthermore, Protectin D1 enhances miRNA-210 expression, activates the PI3K/AKT signaling pathway, and exerts cardioprotective effects. Protectin D1 holds promise for research in cardiovascular diseases and inflammatory disorders .
    Protectin D1

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