Search Result
Results for "
HIF inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
4
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-153017
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-13671
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HIF-1α inhibitor; LW8
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HIF/HIF Prolyl-Hydroxylase
Apoptosis
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Cancer
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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.
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- HY-124875
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HIF inhibitor 64B
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HIF/HIF Prolyl-Hydroxylase
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Neurological Disease
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Arylsulfonamide 64B (HIF inhibitor 64B) is an inhibitor of the hypoxia-induced factor (HIF). Arylsulfonamide 64B inhibits hypoxia/HIF-induced expression of c-Met and CXCR4 and reduces primary tumor growth and metastasis of uveal melanoma mouse model .
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- HY-149260
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- HY-N12840
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Others
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Metabolic Disease
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Logmalicid B is an iridoid glycoside compound that can be isolated from Cornus officinalis and can be used in diabetes research .
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- HY-149491
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TAM Receptor
HIF/HIF Prolyl-Hydroxylase
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Others
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Axl-IN-16 (Compound 4) is a Axl inhibitor. Axl-IN-16 inhibits Axl expression and inhibits the activity of HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 can be isolated from“fruiting liquid (FL)” of Hypholoma lateritium and Hericium erinaceus .
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- HY-151341
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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) .
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- HY-144178
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- HY-149635
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-110266
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GN44028
4 Publications Verification
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-151466
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HIF/HIF Prolyl-Hydroxylase
Monoamine Oxidase
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Cancer
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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 .
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- HY-P10223
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-146144
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-144176
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- HY-P10222
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-P10221
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 KD of 2.6 and 2.2 μM, respectively .
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- HY-19949
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- HY-163370
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- HY-147029
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-18371
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HIF/HIF Prolyl-Hydroxylase
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Inflammation/Immunology
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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 .
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- HY-147813
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- HY-151344
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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) .
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- HY-148860
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-151465
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-P1420
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-115903A
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-136748
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-115903
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-P1420A
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-148264
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- HY-139287
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-125840
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PT2977; MK-6482
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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) .
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- HY-18370
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-130264
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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) .
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- HY-100693
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- HY-149886
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-P2657
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HIF/HIF Prolyl-Hydroxylase
Proton Pump
Endogenous Metabolite
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Cancer
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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.
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- HY-15836
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- HY-12867
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- HY-N0242
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PD-1/PD-L1
HIF/HIF Prolyl-Hydroxylase
STAT
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Inflammation/Immunology
Cancer
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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 .
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- HY-15893
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DMOG
Maximum Cited Publications
47 Publications Verification
Dimethyloxallyl Glycine
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HIF/HIF Prolyl-Hydroxylase
Autophagy
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Cancer
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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 .
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- HY-163512
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HIF/HIF Prolyl-Hydroxylase
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Inflammation/Immunology
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Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body. .
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- HY-101028
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- HY-115746
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- HY-124473
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Naphthafluorescein
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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Naphthofluorescein inhibits the interaction between HIF-1 and Mint3.
Naphthofluorescein suppresses Mint3-dependent HIF-1 activity and glycolysis in cancer cells and macrophages without cytotoxicity in vitro and adverse effect in vivo . Naphthofluorescein is also a fluorescent pH-sensitive probe that can be used for functional Cerenkov imaging .
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- HY-131346
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HIF/HIF Prolyl-Hydroxylase
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Cardiovascular Disease
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HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia .
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- HY-109057A
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JTZ-951 hydrochloride; SAL0951 hydrochloride
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HIF/HIF Prolyl-Hydroxylase
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Metabolic Disease
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Enarodustat hydrochloride is a potent and orally active HIF/HIF Prolyl-Hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat hydrochloride has the potential for renal anemia treatment.
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- HY-156106
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PROTACs
Ligands for E3 Ligase
HIF/HIF Prolyl-Hydroxylase
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Cancer
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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) .
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- HY-146540
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HIF/HIF Prolyl-Hydroxylase
Apoptosis
MDM-2/p53
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Cancer
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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 .
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- HY-15672
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HIF/HIF Prolyl-Hydroxylase
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Neurological Disease
Cancer
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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 .
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- HY-B0219
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Xanthine Oxidase
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Infection
Neurological Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-N0596
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20(R)-Panaxadiol
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PD-1/PD-L1
HIF/HIF Prolyl-Hydroxylase
STAT
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Cancer
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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 .
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- HY-B0219A
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Xanthine Oxidase
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Infection
Neurological Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-123422
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HIF/HIF Prolyl-Hydroxylase
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Cardiovascular Disease
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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) .
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- HY-N10330
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HIF/HIF Prolyl-Hydroxylase
VEGFR
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Cancer
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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 .
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- HY-121172
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM .
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- HY-10231
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- HY-17412S
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Isotope-Labeled Compounds
Antibiotic
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Others
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Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor .
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- HY-N6782
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- HY-13426
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FG-4592
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HIF/HIF Prolyl-Hydroxylase
Ferroptosis
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Cancer
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Roxadustat is an orally active hypoxia-inducible factor (HIF) prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin .
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- HY-153493
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- HY-153493A
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Small Interfering RNA (siRNA)
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Metabolic Disease
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PF-04523655 sodium is a siRNA directed against RTP801 gene. RTP801 sodium is an inhibitor of the mammalian target of rampamycin complex 1 (mTORC1) and downstream transcription factor HIF-1.
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- HY-16031B
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NSC710464 dihydrochloride
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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).
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- HY-119264A
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HIF/HIF Prolyl-Hydroxylase
Ras
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Cancer
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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 .
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- HY-16031
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NSC710464 free base
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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.
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- HY-108697A
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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(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 .
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- HY-106101
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Quinomycin A; NSC-13502
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HIF/HIF Prolyl-Hydroxylase
Antibiotic
Bacterial
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Cancer
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Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM .
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- HY-161427
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HSP
HIF/HIF Prolyl-Hydroxylase
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Cancer
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HSP90-IN-30 (compound 3e) inhibits HSP90 chaperone activity. HSP90-IN-30 inhibits the activity of HIF-1 transcriptional under hypoxia with an IC50 value of 2.16 μM .
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- HY-120087
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-122094
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- HY-18777
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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KC7F2 is a potent hypoxia inducible factor-1 (HIF-1) pathway inhibitor with an IC50 of 20 μM in LN229-HRE-AP cells, and with potential as a cancer therapy agent .
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- HY-44809
-
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HIF/HIF Prolyl-Hydroxylase
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Cardiovascular Disease
Inflammation/Immunology
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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). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1) .
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- HY-158341
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HIF/HIF Prolyl-Hydroxylase
Apoptosis
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Cancer
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IOX5 is a selective prolyl hydroxylases (PHD) inhibitor. IOX5 stabilizes HIF-1α in AML cells, induces apoptosis, and upregulates BNIP3 expression. IOX5 compromises development and progression of acute myeloid leukemia .
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- HY-15468
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-15468A
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HIF/HIF Prolyl-Hydroxylase
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Cardiovascular Disease
Cancer
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IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases .
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- HY-44809A
-
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HIF/HIF Prolyl-Hydroxylase
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Inflammation/Immunology
Cancer
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Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1) .
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- HY-W088075
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Acriflavinium chloride hydrochloride
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HIF/HIF Prolyl-Hydroxylase
Bacterial
SARS-CoV
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Infection
Cancer
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Acriflavine hydrochloride (Acriflavinium chloride hydrochloride) is a fluorescent acridine dye that can be used to label nucleic acid . Acriflavine hydrochloride is an antiseptic. Acriflavine hydrochloride is a potent HIF-1 inhibitor, with antitumor activity. Acriflavine hydrochloride has antimicrobial and antiviral activities . Acriflavine hydrochloride is a potent papain-like protease (PL pro) inhibitor, which inhibits SARS-CoV-2
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- HY-137239
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- HY-120110
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IOX4
5 Publications Verification
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HIF/HIF Prolyl-Hydroxylase
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Neurological Disease
Inflammation/Immunology
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IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2 .
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- HY-16196
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IRC-110160
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Microtubule/Tubulin
HIF/HIF Prolyl-Hydroxylase
STAT
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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.
|
-
- HY-19731
-
MiR-544 inhibitor 1
|
MicroRNA
Apoptosis
|
Cancer
|
SID 3712249 (MiR-544 Inhibitor 1) is a miR-544 biogenesis inhibitor. SID 3712249 binds directly to the precursor miRNA. SID 3712249 blocks production of the mature microRNA and decreases miR-544, HIF-1α, and ATM transcripts. SID 3712249 can be used in the research of cancers, such as breast cancer .
|
-
- HY-161425
-
|
Apoptosis
|
Cancer
|
Antitumor agent-149 (Compound 3) is an analogue of Echinomycin (HY-106101). Antitumor agent-149 inhibits HIF-1α-mediated transcription. Antitumor agent-149 induces cancer cell apoptosis. Antitumor agent-149 inhibits tumor growth in SW620 xenograft mice model .
|
-
- HY-100947
-
|
Ligands for E3 Ligase
|
Others
|
VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology.
|
-
- HY-161313
-
|
Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2 - and GSK126 -resistant of A549 and H460 cells .
|
-
- HY-118543
-
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia. Local administration of TM6089 enhances angiogenesis, and oral administration stimulates HIF activity in transgenic rats expressing a hypoxia-responsive reporter vector .
|
-
- HY-113649
-
|
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 .
|
-
- HY-17412S1
-
|
Isotope-Labeled Compounds
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
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-141625
-
|
HIF/HIF Prolyl-Hydroxylase
|
Others
|
TRC160334 is a hypoxia-inducible factor (HIF) hydroxylase inhibitor. TRC160334 can be used for the research of ischemia/reperfusion injury .
|
-
- HY-107553
-
|
HSP
Apoptosis
|
Cancer
|
Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule .
|
-
- HY-B0223
-
-
- HY-15205
-
STA-9090
|
HSP
Apoptosis
|
Cancer
|
Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 .
|
-
- HY-111387
-
-
- HY-N2425
-
|
Cholinesterase (ChE)
|
Metabolic Disease
|
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 Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system
|
-
- HY-N1477
-
-
- HY-112441
-
-
- HY-16560
-
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-17608
-
GSK1278863
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
Daprodustat (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.
|
-
- HY-103227
-
ZYAN1
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
Desidustat is an orally active HIF hydroxylase inhibitor. Desidustat can be used for the research of various disorders including anemia of different types and conditions associated with ischemia/hypoxia .
|
-
- HY-139993
-
-
- HY-N2199
-
|
Apoptosis
Autophagy
|
Cancer
|
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits migration and invasion of A549 cells by reversing EMT, and induces cell apoptosis and autophagy. Sotetsuflavone inhibits HIF-1α, VEGF, angiostatin, MMP-9, and MMP-13 expression in A549 cells. Sotetsuflavone also protects mice against Crohn's disease (CD)-like colitis. Sotetsuflavone can be used for research of NSCLC .
|
-
- HY-101449
-
|
HIF/HIF Prolyl-Hydroxylase
|
Metabolic Disease
|
Adaptaquin is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PHD2), with an IC50 of 2 μM. Adaptaquin can inhibit lipid peroxidation and maintain mitochondrial function .
|
-
- HY-101023
-
-
- HY-17412
-
-
- HY-17412A
-
-
- HY-N12041
-
|
TAM Receptor
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression .
|
-
- HY-148877
-
|
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) .
|
-
- HY-12654
-
BAY 85-3934
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
Molidustat (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.
|
-
- HY-16560S
-
Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5
|
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
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-19357
-
-
- HY-110282
-
|
Oxidative Phosphorylation
Mitochondrial Metabolism
|
Metabolic Disease
|
S3QEL-2, a suppressor of superoxide production from mitochondrial complex III, potently and selectively suppresses site IIIQo superoxide production (IC50=1.7 μM). S3QEL-2 does not affect oxidative phosphorylation, and normal electron flux. S3QEL-2 inhibits HIF-1α accumulation .
|
-
- HY-N6030
-
(Rac)-Dencichin; (Rac)-ODAP
|
HIF/HIF Prolyl-Hydroxylase
|
Others
|
(Rac)-Dencichine ((Rac)-Dencichin) is the racemate of Dencichin. Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity .
|
-
- HY-117479
-
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
CL67 is a potent hypoxia-inducible factor (HIF) pathway inhibitor. CL67 interferes G-quadruplex structures within promoter sequences. CL67 can be used in research of renal cancer .
|
-
- HY-17412R
-
-
- HY-16187
-
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
|
Cancer
|
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 .
|
-
- HY-124722
-
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
OHM1 is an analog of HIF1α CTAD that inhibits its binding with p300/CBP. OHM1 targets CH1 domain with an affinity of 0.53 μM .
|
-
- HY-155009
-
|
HIF/HIF Prolyl-Hydroxylase
|
Others
|
PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research .
|
-
- HY-101277
-
PG-1016548; AKB-6548
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor . Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo .
|
-
- HY-100947A
-
|
Ligands for E3 Ligase
|
Others
|
cis VH-298 is a cis-form of VH-298 (HY-100947). VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology .
|
-
- HY-N0234
-
7-O-Methylbavachin; Bavachinin A
|
Amyloid-β
PPAR
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
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
-
4-Caffeoylquinic acid; 4-O-Caffeoylquinic acid
|
Endogenous Metabolite
NF-κB
Keap1-Nrf2
mTOR
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
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 .
|
-
- HY-13426S
-
|
HIF/HIF Prolyl-Hydroxylase
Ferroptosis
|
Cancer
|
Roxadustat-d5 is deuterium labeled Roxadustat. Roxadustat is an oral hypoxia-inducible factor prolyl-hydroxylase inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin[1].
|
-
- HY-W009156
-
-
- HY-B1295
-
-
- HY-15641
-
FG-2216
3 Publications Verification
IOX3; YM311
|
HIF/HIF Prolyl-Hydroxylase
|
Metabolic Disease
|
FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo .
|
-
- HY-B2171A
-
Carminomycin hydrochloride; Carminomicin I hydrochloride
|
Apoptosis
|
Infection
Cancer
|
Carubicin hydrochloride is a microbially-derived compound. Carubicin hydrochloride is an effective inhibitor of VHL-defective (VHL−/−) CCRCC cell proliferation. Carubicin hydrochloride also induces apoptosis by a mechanism independent of p53 or hypoxia-inducible factor HIF2. Carubicin hydrochloride has the potential for the research of cancer diseases .
|
-
- HY-B2171
-
Carminomycin; Carminomicin I
|
Apoptosis
|
Infection
Cancer
|
Carubicin (Carminomycin) is a microbially-derived compound. Carubicin is an effective inhibitor of VHL-defective (VHL−/−) CCRCC cell proliferation. Carubicin also induces apoptosis by a mechanism independent of p53 or hypoxia-inducible factor HIF2. Carubicin has the potential for the research of cancer diseases .
|
-
- HY-10450
-
BMS-512148
|
SGLT
|
Metabolic Disease
Cancer
|
Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-120217
-
VH032
3 Publications Verification
|
Ligands for E3 Ligase
|
Cancer
|
VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kd
|
-
- HY-155721
-
22-(4′-Pyridinecarbonyl) jorunnamycin A
|
Akt
mTOR
|
Cancer
|
22-(4′-py)-JA is a semisynthetic derivative of junamycin A (JA) that can be isolated from the Thai blue sponge (Xestospongia sp.). 22-(4′-py)-JA has antimetastatic activity and can inhibit AKT/mTOR/p70S6K signaling. 22-(4′-py)-JA inhibits tumor cell invasion and tube formation in human umbilical vein endothelial cells (HUVEC), downregulates metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α) and vascular endothelial growth factor (VEGF). 22-(4′-py)-JA has potent anticancer activity against non-small cell lung cancer (NSCLC) .
|
-
- HY-128872
-
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 .
|
-
- HY-136300
-
-
- HY-138678
-
|
Ligands for E3 Ligase
|
Cancer
|
(R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669) .
|
-
- HY-136055
-
VH032-C5-COOH
|
E3 Ligase Ligand-Linker Conjugates
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
(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 .
|
-
- HY-120793
-
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 .
|
-
- HY-10450A
-
BMS-512148 (2S)-1,2-propanediol, hydrate
|
SGLT
|
Metabolic Disease
Cancer
|
Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-B1295
-
Litarex tetrahydrate
|
Biochemical Assay Reagents
|
Lithium citrate (Litarex) tetrahydrate is the major active ingredient of Garcinia cambogia. Lithium citrate tetrahydrate competitively inhibits ATP citrate lyase with weight loss benefits. Lithium citrate tetrahydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1420
-
|
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 .
|
-
- HY-P10223
-
|
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 .
|
-
- HY-P10222
-
|
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 .
|
-
- HY-P10221
-
|
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 KD of 2.6 and 2.2 μM, respectively .
|
-
- HY-P1420A
-
|
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 .
|
-
- HY-P5908
-
-
- HY-P2657
-
|
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.
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17412S1
-
|
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 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-13426S
-
|
Roxadustat-d5 is deuterium labeled Roxadustat. Roxadustat is an oral hypoxia-inducible factor prolyl-hydroxylase inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin[1].
|
-
-
- HY-17412S
-
|
Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor .
|
-
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