HIF
Hypoxia inducible factors (HIFs) are heterodimeric proteins belonging to the basic helix-loop-helix-PAS (bHLH/PAS) family of transcription factors that mediate the primary transcriptional response to stress caused by hypoxia (accessible O2 level < 2%). HIFs are characterized by containing two subunits, including O2-labile α subunit (HIFα) and constitutively expressed β subnit (HIFβ). Mammalian HIFα consists of three isoforms, including HIF1α, HIF2α and HIF3α, which play an essential role in the regulation of HIF activity by O2 availability. Under normal O2 tension, HIFα is hydroxylated at the two conserved proline residues within the O2-dependent degradation (ODD) domain by prolylhydroxylase domain proteins (PHDs) and undergoes proteosomal degradation catalyzed by a complex formed by E3 ubiquitin ligase and the von Hippel-Lindau protein (pVHL); while, under hypoxia, HIFα stabilizes with PHDs being deactivated and hence induce transcription of genes with adaptive functions.
Products for HIF
- Cat.No. Product Name Information
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GC69794
(Rac)-Arnebin 1
(Rac)-Arnebin 1 is the racemic form of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. These compounds are naphthoquinones isolated from plants in the Lithospermum genus, with β,β-Dimethylacrylshikonin exhibiting anti-tumor activity.
- GC65133 (S,R,S)-AHPC-C5-COOH (S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized?E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases.
- GC61949 1,4-DPCA ethyl ester 1,4-DPCA ethyl ester is the ethyl ester of 1,4-DPCA and can inhibit factor inhibiting HIF (FIH).
- GC16195 2,4-DPD Diethyl pyridine-2,4-dicarb is a potent prolyl 4-hydroxylase-directed proinhibitor.
- GC15084 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2/2-Me) is a HIF-1α inhibitor that inhibits HIF-1α accumulation and HIF transcriptional activity. 2-Methoxyestradiol can trigger p53-induced apoptosis and has potential antitumor activity..
- GC14282 3-acetyl-11-keto-β-Boswellic Acid 3-acetyl-11-keto-β-Boswellic Acid (Acetyl-11-keto-β-boswellic acid) is an active triterpenoid compound from the extract of Boswellia serrate and a novel Nrf2 activator.
- GC35230 Acetylarenobufagin Acetylarenobufagin is a steroidal hypoxia inducible factor-1 (HIF-I) modulator.
- GC32083 Acriflavine Acriflavine is a fluorescent dye for labeling high molecular weight RNA.
- GC62354 Acriflavine hydrochloride Acriflavine hydrochloride (Acriflavinium chloride hydrochloride) is a fluorescent acridine dye that can be used to label nucleic acid.
- GC12487 Adaptaquin HIF-prolyl hydroxylase-2 (PHD2) inhibitor
- GC33416 AFP464 AFP464 (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.
- GC62277 AKB-6899 Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects.
- GC42785 Amifostine (hydrate) Amifostine (hydrate) (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine (hydrate) selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine (hydrate) is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine (hydrate) protects cells from damage by scavenging oxygen-derived free radicals. Amifostine (hydrate) reduces renal toxicity and has antiangiogenic action.
- GC12698 BAY 87-2243 A HIF-1 inhibitor,potent and selective
- GC17405 Chetomin An inhibitor of HIF signaling
- GN10518 Chitosamine hydrochloride
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GN10308
Chlorogenic acid
Chlorogenic acid is a major phenolic compound in coffee and tea.
- GC16647 Daprodustat(GSK1278863) Daprodustat(GSK1278863) (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease.
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GC68955
Deferoxamine
Deferoxamine (Deferoxamine B) is an iron chelator (binding Fe(III) and many other metal cations), widely used to reduce the accumulation and deposition of iron in tissues.
- GC31230 Dencichin (Dencichine) Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity.
- GC38767 Deoxyshikonin A natural products with anti-tumor activity
- GC32449 Desidustat An inhibitor of HIF-PH
- GC18236 Echinomycin An inhibitor of HIF1mediated gene transcription
- GC33043 EL-102 EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer.
- GC33634 Enarodustat (JTZ-951) Enarodustat (JTZ-951) is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM.
- GC33170 ENMD-119 (ENMD 1198) ENMD-119 (ENMD 1198) (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-119 (ENMD 1198) is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
- GC61669 Ethyl 3,4-dihydroxybenzoate Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds.
- GC13139 FG-4592 (ASP1517) An inhibitor of HIF-PH enzymes
- GC16638 FG2216 HIF-prolyl hydroxylase inhibitor
- GC50537 FM19G11 A HIF α-subunit inhibitor
- GC38044 Fraxinellone
- GC30263 Glucosamine (D-Glucosamine) Glucosamine (D-Glucosamine) (D-Glucosamine (D-Glucosamine)) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement.
- GN10669 Glucosamine sulfate
- GC34595 GN44028 A HIF-1 inhibitor
- GC40918 Gramicidin A Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B.
- GC39146 HIF-1 inhibitor-1 An inhibitor of HIF-1 signaling
- GC66464 HIF-1α-IN-2 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.
- GC62584 HIF-2α-IN-2 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).
- GC62418 HIF-2α-IN-3 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.
- GC63678 HIF-2α-IN-4 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.
- GC31358 HIF-2α-IN-1 HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay.
- GC67941 HIF-PHD-IN-1
- GC65570 HIF1-IN-3 HIF1-IN-3 (compound F4) is a potent HIF1 inhibitor with an EC50 value of 0.9 μM. HIF1-IN-3 can be used for researching anticancer.
- GC11767 Hydralazine HCl Hydralazine HCl is a orally active antihypertensive agent, reduces peripheral resistance directly by relaxing the smooth muscle cell layer in arterial vessel.
- GC60919 Hydroxycitric acid tripotassium hydrate Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia.
- GC32948 IDF-11774 A novel HIF-1 inhibitor
- GC13018 IOX2(Glycine) A selective PHD2 inhibitor
- GC12255 IOX4 PHD2 inhibitor
- GC63828 Izilendustat Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2).
- GC15379 JNJ-42041935 Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor
- GC13141 KC7F2 An inhibitor of HIF-1a protein synthesis
- GC32724 LW6 (HIF-1α inhibitor) LW6 (HIF-1α inhibitor) (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 (HIF-1α inhibitor) decreases HIF-1α protein expression without affecting HIF-1β expression.
- GC64945 M1001 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.
- GC65046 M1002 M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors.
- GC19251 MK-8617 MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.
- GC14319 ML 228 A HIF pathway activator
- GC10046 Molidustat (BAY85-3934) Molidustat (BAY85-3934) (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3.
- GC62406 Moracin O Moracin O is a 2-arylbenzofuran isolated from the Mori Cortex Radicis.
- GC17358 Octyl-α-ketoglutarate prolyl hydroxylases (PHD) activator
- GC12821 Oltipraz Nrf2 activator;An antischistosomal agent
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GC41625
Oroxylin A
Oroxylin A is a flavonoid that has been found in S.
- GN10452 Paeoniflorin
- GC64584 PHD-1-IN-1 PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM.
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GC41572
PRLX-93936
PRLX-93936 is an analog of erastin that has antitumor activity.
- GC32680 PT-2385 PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.
- GC65333 PT2399 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.
- GC37034 PT2977 PT2977 (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. PT2977, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. PT2977 is a potential treatment for clear cell renal cell carcinoma (ccRCC).
- GC11031 PX-478 2HCl PX-478 is a selective inhibitor that suppresses constitutive and hypoxia-induced HIF-1α levels.
- GC37066 Rac-PT2399 A potent and specific HIF-2α inhibitor
- GC49190 Roxadustat-d5 An internal standard for the quantification of roxadustat
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GC69956
Steppogenin
Steppogenin is an effective inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be used for research on angiogenesis-related diseases such as solid tumors.
- GC32876 SYP-5 A HIF-1 inhibitor
- GC50211 TAT-cyclo-CLLFVY Selective HIF-1 dimerization inhibitor
- GC50128 TC-S 7009 High affinity and selective HIF-2α inhibitor
- GC32945 THS-044 THS-044 binding stabilizes the HIF2α PAS-B folded state, for regulating HIF2 activity in endogenous and clinical settings.
- GC32228 Tilorone dihydrochloride An interferon-inducing antiviral agent
- GC49062 Tiopronin-d3 An internal standard for the quantification of tiopronin
- GC37801 TM6089 TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia.
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GC31498
TP0463518
TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor
- GC64001 TRC160334 TRC160334 is a hypoxia-inducible factor (HIF) hydroxylase inhibitor.
- GC16811 Vadadustat HIF-PH inhibitor
- GC37889 VCE-004.8 VCE-004.8 (VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist.
- GC61863 Verucopeptin 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.
- GC37966 ZINC13466751 ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 ?M.