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Isoforms Recommended: HIF
Results for "

HIF-2α

" in MedChemExpress (MCE) Product Catalog:

53

Inhibitors & Agonists

4

Peptides

2

Natural
Products

1

Isotope-Labeled Compounds

4

Antibodies

2

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-125840
    Belzutifan
    10+ Cited Publications

    PT2977; MK-6482

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC) .
    Belzutifan
  • HY-B0219
    Allopurinol
    10+ Cited Publications

    		 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 [2] .
    Allopurinol
  • HY-12867
    PT-2385
    Maximum Cited Publications
    52 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM [2].
    PT-2385
  • HY-111431
    p-Cresyl sulfate
    5+ Cited Publications

    p-Tolyl sulfate

    		 JNK p38 MAPK Reactive Oxygen Species (ROS) 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 [2] .
    p-Cresyl sulfate
  • HY-108697
    PT2399
    10+ Cited Publications

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo [2] .
    PT2399
  • HY-B0219A
    Allopurinol sodium
    10+ Cited Publications

    		 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 [2] .
    Allopurinol sodium
  • 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 (KD = 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 .
    THS-044
  • HY-159644
    Casdatifan

    AB521

    		 HIF/HIF Prolyl-Hydroxylase VEGFR Cancer
    Casdatifan (AB521) is an orally active and selective allosteric small-molecule inhibitor of hypoxia-inducible factor 2α (HIF-2α). Casdatifan inhibits pro-tumor gene transcription by blocking the heterodimerization of HIF-2α with ARNT, and significantly suppresses tumor growth in clear cell renal cell carcinoma (ccRCC) models either as a monotherapy or in combination with agents such as Zimberelimab (HY-P99109). Casdatifan is applicable for the research of ccRCC .
    Casdatifan
  • HY-18371
    TC-S 7009
    1 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ? 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression [2].
    TC-S 7009
  • HY-153016
    HIF-2α agonist 2
    1 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    HIF-2α agonist 2 (compound 10) is a HIF-2α agonist with an EC50 value of 1.68 μM at the dose of 20 μM. HIF-2α agonist 2 is non-cytotoxic against 786-O-HRE-Luc cells. HIF-2α agonist 2 can be used for oxygen metabolism research .
    HIF-2α agonist 2
  • 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 [2].
    Izilendustat
  • HY-148860
    NVP-DFF332

    HIF-2α-IN-8

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity .
    NVP-DFF332
  • HY-111547
    M1001

    		HIF/HIF Prolyl-Hydroxylase Cancer
    M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research .
    M1001
  • HY-19949
    HIF-2α-IN-1
    1 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    HIF-2α-IN-1 (compound 9b) is a HIF-2α inhibitor (IC50=1.7 μM, SPA/scintillation proximity assay) .
    HIF-2α-IN-1
  • HY-136748
    HIF-2α-IN-4
    1 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing .
    HIF-2α-IN-4
  • HY-113649
    AKB-6899
    2 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects .
    AKB-6899
  • HY-P10221A
    Cyclo(CKLIIF) TFA

    		HIF/HIF Prolyl-Hydroxylase Cancer
    Cyclo(CKLIIF) TFA is an inhibitor of HIF-1α and HIF-2α. The KD values of Cyclo(CKLIIF) TFA for the PAS-B domains of HIF1-α and HIF2-α are 2.6 μM and 2.2 μM, respectively. Cyclo(CKLIIF) TFA disrupts the protein-protein interaction between HIF-1α and HIF-1β. Cyclo(CKLIIF) TFA can be used in cancer research .
    Cyclo(CKLIIF) TFA
  • HY-147426
    Zifcasiran

    ADS-007; ARO HIF2

    		 Small Interfering RNA (siRNA) HIF/HIF Prolyl-Hydroxylase Cancer
    Zifcasiran (ADS-007; ARO HIF2) is an siRNA synthetic double-stranded RNAi trigger. Zifcasiran sodium selectively target hypoxia-inducible factor-2α (HIF2α) interrupting downstream pro-oncogenic signaling in clear cell renal cell carcinoma (ccRCC). Zifcasiran sodium engages the cell's RNAi machinery to target HIF2α (EPAS1) mRNA for degradation, thereby reducing the amount of free HIF2α mRNA available for translation .
    Zifcasiran
  • HY-B0219R
    Allopurinol (Standard)

    		Reference Standards Xanthine Oxidase Infection Neurological Disease Inflammation/Immunology Cancer
    Allopurinol (Standard) is the analytical standard of Allopurinol. This product is intended for research and analytical applications. 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 [2] .
    Allopurinol (Standard)
  • HY-177078
    Davotifan

    		HIF/HIF Prolyl-Hydroxylase Cancer
    Davotifan (Compound A17) is a bicyclic compound. Davotifan is an inhibitor of HIF-2α. Davotifan can be studied in research for HIF-2α-related cancer .
    Davotifan
  • HY-125840R
    Belzutifan (Standard)

    PT2977 (Standard); MK-6482 (Standard)

    		 HIF/HIF Prolyl-Hydroxylase Reference Standards Cancer
    Belzutifan (Standard) is the analytical standard of Belzutifan. This product is intended for research and analytical applications. Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC) .
    Belzutifan (Standard)
  • 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 KD of 14.5 and 10.2 μM, respectively .
    Cyclo(CRLLIF)
  • 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 [2] .
    CMC2.24
  • HY-108697A
    (Rac)-PT2399

    		HIF/HIF Prolyl-Hydroxylase Cancer
    (Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM .
    (Rac)-PT2399
  • HY-148264
    Imdatifan

    HIF-2α-IN-7

    		 HIF/HIF Prolyl-Hydroxylase Infection Metabolic Disease Inflammation/Immunology Cancer
    Imdatifan (HIF-2α-IN-7) is a hypoxia inducible factor 2α (HIF-2α) inhibitor. Imdatifan can inhibit HIF-2α with an EC50 value of 6 nM. Imdatifan can be used for the research of various types of diseases including cancer, liver disease, inflammatory disease, pulmonary diseases and iron load disorders .
    Imdatifan
  • HY-16191
    ELR510444
    1 Publications Verification

    		 Microtubule/Tubulin Apoptosis HIF/HIF Prolyl-Hydroxylase Mitosis Cancer
    ELR510444 is an orally active tubulin inhibitor with an IC50 of 10 μM. ELR510444 binds to the colchicine-binding site on β-tubulin, inhibits tubulin assembly, depolymerizes microtubules and blocks HIF activity. ELR510444 induces cellular microtubule loss, abnormal mitotic spindle, mitotic arrest, apoptosis, morphological changes in tumor endothelial cells, and inhibits cancer cell proliferation, angiogenesis and tumor growth. ELR510444 can be used in research related to various cancers such as renal cell carcinoma [2].
    ELR510444
  • HY-18370
    HIF-2α-IN-3

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent .
    HIF-2α-IN-3
  • HY-161265
    HIF-2α agonist 3

    		HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    HIF-2α agonist 3 (Compound 14d) is an orally active HIF-2α agonist with a EC50 value of 1.78 μM. HIF-2α agonist 3 can be used in the study of renal anemia .
    HIF-2α agonist 3
  • HY-147426A
    Zifcasiran sodium

    ADS-007 sodium; ARO HIF2 sodium

    		 Small Interfering RNA (siRNA) HIF/HIF Prolyl-Hydroxylase Cancer
    Zifcasiran (ADS-007) sodium is an siRNA synthetic double-stranded RNAi trigger. Zifcasiran sodium selectively target hypoxia-inducible factor-2α (HIF2α) interrupting downstream pro-oncogenic signaling in clear cell renal cell carcinoma (ccRCC). Zifcasiran sodium engages the cell's RNAi machinery to target HIF2α (EPAS1) mRNA for degradation, thereby reducing the amount of free HIF2α mRNA available for translation .
    Zifcasiran sodium
  • HY-130264
    HIF-2α-IN-2

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA) .
    HIF-2α-IN-2
  • HY-B0219S1
    Allopurinol-13C,15N2

    		Isotope-Labeled Compounds Xanthine Oxidase Infection Neurological Disease Inflammation/Immunology Cancer
    Allopurinol- 13C, 15N2 is the 13C- and 15N-labeled labeled Allopurinol (HY-B0219). 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 [2] .
    Allopurinol-13C,15N2
  • HY-111431AR
    p-Cresyl sulfate potassium (Standard)

    p-Tolyl sulfate potassium (Standard)

    		 JNK p38 MAPK Reactive Oxygen Species (ROS) Reference Standards Metabolic Disease
    p-Cresyl sulfate (potassium) (Standard) is the analytical standard of p-Cresyl sulfate (potassium). This product is intended for research and analytical applications. p-Cresyl sulfate (p-Tolyl sulfate) potassium is a uremic toxin, that can cause renal damage and dysfunction. p-Cresyl sulfate potassium shows antiproliferation activity. p-Cresyl sulfate potassium increases the protein expression of HIF-1α and VHL, decreases the protein expression of HIF-2α. p-Cresyl sulfate potassium induces epithelial-mesenchymal transition (EMT). p-Cresyl sulfate potassium activates the JNK and p38 MAPK signaling pathways [2] .
    p-Cresyl sulfate potassium (Standard)
  • 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 KD of 65 and 123 μM, respectively .
    Cyclo(CRVIIF)
  • HY-144178
    HIF-2α-IN-6

    		HIF/HIF Prolyl-Hydroxylase Others
    HIF-2α-IN-6 (117) is a HIF-2α inhibitor .
    HIF-2α-IN-6
  • HY-144176
    HIF-2α-IN-5

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of < 50 nM .
    HIF-2α-IN-5
  • HY-163598
    HIF-2α-IN-11

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-11 (1) is a HIF-2α inhibitor, with an IC50 of 59.2 nM .
    HIF-2α-IN-11
  • HY-163601
    HIF-2α-IN-14

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-14 (18) is a HIF-2α inhibitor, with an IC50 of 0.27 μM .
    HIF-2α-IN-14
  • HY-163602
    HIF-2α-IN-15

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-15 (35) is a HIF-2α inhibitor, with an IC50 of 0.41 μM .
    HIF-2α-IN-15
  • HY-163600
    HIF-2α-IN-13

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-13 (18) is a HIF-2α inhibitor, with an IC50 of 2.7 μM .
    HIF-2α-IN-13
  • HY-163599
    HIF-2α-IN-12

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-12 (9) is a HIF-2α inhibitor, with an IC50 of 0.9 μM .
    HIF-2α-IN-12
  • HY-163597
    HIF-2α-IN-10

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-10 (17) is a HIF-2α inhibitor, with an IC50 of 0.05 μM .
    HIF-2α-IN-10
  • HY-163603
    HIF-2α-IN-16

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-16 (48) is a HIF-2α inhibitor, with an IC50 of 0.091 μM .
    HIF-2α-IN-16
  • HY-183583
    HIF-2α-IN-18

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-18 is a selective HIF-2α inhibitor with a human IC50 of 8.1 nM. HIF-2α-IN-18 binds to the HIF-2α PAS-B domain, induces conformational perturbations at the HIF-2α/ARNT dimerization interface, destabilizes the HIF-2α/ARNT heterodimer, and blocks HIF-2α-mediated transcriptional activity. HIF-2α-IN-18 inhibits hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1, without inhibiting HIF-1α target genes PGK1 and PDK1. HIF-2α-IN-18 can be used for the research of clear cell renal cell carcinoma, hepatocellular carcinoma[1].
    HIF-2α-IN-18
  • HY-149886
    HIF-2α-IN-9

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-9 (compound 35r) is an inhibitor ofHIF-2α. HIF-2α-IN-9 inhibits VEGF-A (IC50=305 nM), and regulates growth-promoting genes in tumor cells, reactivates macrophage-mediated tumor immunity .
    HIF-2α-IN-9
  • HY-W470101
    HIF-2α-IN-17

    		HIF/HIF Prolyl-Hydroxylase Apoptosis HSP Caspase Cancer
    HIF-2α-IN-17 is a selective hypoxia-inducible factor 2α (HIF2α) inhibitor that binds to the PAS-B domain of HIF2α. HIF-2α-IN-17 disrupts the interaction between HIF2α and the molecular chaperone Hsp70, leading to proteasomal degradation of HIF2α. HIF-2α-IN-17 exhibits antitumor activity and induces apoptosis in cancer cells. HIF-2α-IN-17 is applicable for research on cancers such as clear cell renal cell carcinoma .
    HIF-2α-IN-17
  • 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) .
    HIF-1/2α-IN-1
  • HY-139855
    ZG-2033

    		HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    ZG-2033 (Compound 26) is an orally active HIF-2α agonist that demonstrates nanomolar activity in luciferase reporter gene assays (EC50 = 490 nM). ZG-2033 has the effect of alleviating anemia and exhibits synergistic action with AKB-6548 (HY-101277) in anemia, and can be used in the study of renal anemia .
    ZG-2033
  • 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 [2].
    Izilendustat hydrochloride
  • 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 .
    dCNP
  • HY-179647
    ZG-2686

    		HIF/HIF Prolyl-Hydroxylase Metabolic Disease Endocrinology
    ZG-2686 is a potent and selective HIF-2α agonist with an EC50 of 0.25 µM. ZG-2686 exhibits selectivity over PHD2. ZG-2686 binds to a specific internal cavity of HIF-2α, forming hydrogen bonds via structural water molecules, which stabilizes the HIF-2α/β heterodimer and enhances transcriptional activity. ZG-2686 synergizes with Vadadustat (HY-101277) to upregulate HIF-2α-dependent EPO gene expression both in vitro and in vivo. ZG-2686 can be used for the research of renal anemia .
    ZG-2686

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