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Catalog No.
Product Name
Application
Product Information
Citations
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HIF-PH inhibitor
DMOG is a cell permeable, competitive inhibitor of HIF-PH. It acts to stabilize HIF-1α expression at normal oxygen tensions in cultured cells, at concentrations between 0.1 and 1 mM.- Hideaki Nakamura, .et al. , PLoS One, 2018, 13(2): e0192136 PMID: 29466367
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HIF-prolyl hydroxylase Inhibitor
GSK1278863 is a novel HIF-prolyl hydroxylase inhibitor.- Masaki Murao, .et al. , Int. J. Mol. Sci., 2025, 26(6), 2742 PMID: 40141384
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HIF-PHs inhibitor
FG-4592 is a novel hypoxia inducible factor prolyl hydroxylase inhibitor, in CKD anemia.- Masaki Murao, .et al. , Int. J. Mol. Sci., 2025, 26(6), 2742 PMID: 40141384
- Weilin Song, .et al. , Biomedicines, 2022, Dec 23;11(1):37 PMID: 36672545
- Singh C, .et al. , JCI Insight, 2019, Jul 25;4(14) PMID: 31341109
- Hideaki Nakamura, .et al. , PLoS One, 2018, 13(2): e0192136 PMID: 29466367
- Singh C, .et al. , Invest Ophthalmol Vis Sci, 2018, Jul 2;59(8):3440-3448 PMID: 30025089
- George Hoppe, .et al. , Proc Natl Acad Sci U S A, 2016, May 3; 113(18): E2516-E2525 PMID: 27091985
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HIF-PHD inhibitor
IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. -
HIF-1α inhibitor
Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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HIF-1α/von Hippel-Lindau interaction inhibitor
ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 ?M. -
HIF inhibitor
BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. -
HIF-1α inhibitor
Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that controls genes involved in glycolysis, angiogenesis, migration, and invasion. Echinomycin is a cell-permeable inhibitor of HIF-1-mediated gene transcription -
HIF-1alpha inhibitor
PX-478 is HIF-1alpha inhibitor, is also an orally active small molecule with potential antineoplastic activity. PX-478 has excellent activity against established human tumor xenografts, providing tumor regressions with prolonged growth delays which correlate positively with HIF-1 levels. PX-478 is a highly water soluble molecule, with good i.v., i.p. and p.o. antitumor activity. -
HIF-PH inhibitor
Molidustat is a novel inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) which stimulates erythropoietin (EPO) production and the formation of red blood cells. -
HIF-PHD Inhibitor II
JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes. -
HIF-2a translation inhibitor
HIF-2a translation inhibitor (IC50 value 5 uM); Decreases HIF-2a protein and HIF-2a target gene expression in normoxia and hypoxia independent of HIF-2a mRNA expression or HIF-2a protein stability, and independent of mTOR activity. Moreover, the translation inhibitor 76 enhances binding of IRP1 to the HIF-2a IRE (Iron-Responsive Element). -
HIF prolyl-hydroxylase inhibitor
Vadadustat, also known as AKB-6548 and PG-1016548, is a potent Hypoxia-inducible factor-proline dioxygenase inhibitor. -
HIF hydroxylase inhibitor
Desidustat is an antianaemic drug candidate. It is an inhibitor of HIF hydroxylase extracted from patent WO 2014102818 A1, compound example 2. -
HIF-2α inhibitor
HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay. IC50 value: ?? 500 nM Target: HIF-2α. -
HIF-1α inhibitor
AFP464, is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator. -
HIF-2α inhibitor
(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. -
HIF-PHD inhibitor
Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM. Antianemia agent. -
Pan-PPAR Agonist, HIF-1α Inhibitor
Bavachinin is a pan-peroxisome proliferator-activated receptor (PPAR) agonist and a HIF-1α inhibitor, demonstrating IC50 values of 21.043 μM, 12.819 μM, and 0.622 μM for PPAR-α, PPAR-β/δ, and PPAR-γ, respectively. This compound exhibits significant antitumor activity against non-small cell lung cancer through its modulation of PPAR-γ. Additionally, Bavachinin possesses notable anti-inflammatory and anti-angiogenic properties, making it a valuable tool for research in cancer and metabolic disorders. Its oral bioavailability further supports its utility in various biological studies. -
HIF-PHDs Inhibitor
Adaptaquin is a blood-brain barrier (BBB)-penetrable inhibitor of hypoxia-inducible factor prolyl hydroxylases (HIF-PHDs). It exhibits anti-inflammatory and neuroprotective properties, effectively inhibiting lipid peroxidation and preserving mitochondrial function while reducing neuronal cell death. Adaptaquin is a valuable research tool for studying neurological disorders, including Parkinson's disease. -
HIF-1 Inhibitor
Moracin O is a selective inhibitor of hypoxia-inducible factor-1 (HIF-1) derived from Morus alba Linn. It demonstrates significant in vitro activity in inhibiting HIF-1, effectively reducing reactive oxygen species (ROS) production induced by oxygen-glucose deprivation (OGD). This compound is valuable for research into neuroprotection and anti-inflammatory effects, making it suitable for studies on cellular responses to hypoxic conditions. -
HIF-1α Inhibitor
O-Carboranylphenoxyacetanilide functions as a HIF-1α inhibitor, effectively blocking the activation of HIF-1α. This compound demonstrates significant inhibition of HIF transcriptional activity in HeLa cells, with an IC50 value of 0.74 μM. Additionally, O-Carboranylphenoxyacetanilide targets HSP60, impairing both its chaperone and ATPase activities, making it a valuable reagent for research on hypoxia-regulated pathways and cellular stress responses. -
HIF-1α Inhibitor
GEM-5 is a gemcitabine-based conjugate that functions as a potent HIF-1α inhibitor, with an IC50 value of 30 nM. This compound effectively down-regulates HIF-1α expression while promoting the up-regulation of the tumor suppressor protein p53. GEM-5 has demonstrated the ability to induce apoptosis in A2780 cancer cells and inhibit tumor growth, making it a valuable tool for cancer research and therapeutic studies targeting hypoxia-driven tumor progression. -
ROS/HIF-1α Inhibitor
Terpestacin is a potent inhibitor of reactive oxygen species (ROS) production and a negative regulator of hypoxia-inducible factor 1-alpha (HIF-1α). Derived from Phoma exigua var. heteromorpha, Terpestacin binds to UQCRB, effectively impeding mitochondrial ROS generation. Its demonstrated ability to inhibit tumor angiogenesis in the FM3A breast cancer cell xenograft model highlights its relevance in cancer research, while also exhibiting notable antitumor and phytotoxic activities. -
HIF-1 Inhibitor
Cyclo(CLLFVY) is a selective inhibitor of hypoxia-inducible factor-1 (HIF-1), demonstrating IC50 values of 19 μM in U2OS cells and 16 μM in MCF-7 cells. By binding to the PAS-B domain of HIF-1α, cyclo(CLLFVY) effectively disrupts HIF-1 dimerization and subsequent transcriptional activity. This compound downregulates the expression of key hypoxia response genes, including VEGF and CAIX, and shows potential for antitumor applications in HIF-1 associated cancers. -
HIF-2α Inhibitor
Casdatifan is an orally bioavailable allosteric inhibitor targeting hypoxia-inducible factor 2α (HIF-2α). It functions by preventing the heterodimerization of HIF-2α with ARNT, thereby inhibiting pro-tumor gene transcription. Casdatifan has demonstrated significant tumor growth suppression in clear cell renal cell carcinoma (ccRCC) models, both as a single agent and in combination therapies. This reagent is valuable for research related to ccRCC and HIF-2α signaling pathways. -
HIF-1α Inhibitor
7-Hydroxyneolamellarin A is a potent inhibitor of hypoxia-inducible factor-1α (HIF-1α), a key regulator of cellular responses to low oxygen levels. Derived from the sponge Dendrilla nigra, this natural product effectively reduces HIF-1α protein accumulation and suppresses its transcriptional activity on vascular endothelial growth factor (VEGF). Research applications of 7-Hydroxyneolamellarin A include investigations into cancer biology and the modulation of tumor microenvironments. -
RAF-1/HIF-1α Inhibitor
MO-2097 is a selective RAF-1 and HIF-1α inhibitor that induces the destabilization of RAF-1, resulting in decreased levels of epithelial-mesenchymal transition (EMT) transcription factors and mesenchymal markers. Additionally, MO-2097 effectively inhibits HIF-1α protein expression mediated by hnRNPA2B1 in hypoxic conditions. This compound promotes the generation of mitochondrial reactive oxygen species (ROS), contributing to apoptosis in malignant cells. MO-2097 demonstrates significant potential in suppressing colorectal cancer metastasis by targeting the RAF/MEK/ERK signaling pathway and has shown efficacy in reducing tumor growth in HCT116 cell xenograft mouse models, thus serving as a valuable tool for colorectal cancer research. -
HIF2α Inhibitor
HIF-2α-IN-17 is a selective inhibitor of hypoxia-inducible factor 2α (HIF2α) that targets the PAS-B domain, effectively disrupting its interaction with the molecular chaperone Hsp70. This interference promotes the proteasomal degradation of HIF2α, leading to significant antitumor activity and the induction of apoptosis in cancer cells. HIF-2α-IN-17 is primarily utilized in research focused on malignancies such as clear cell renal cell carcinoma. -
HIF-1α/Glutamate Inhibitor
Minocycline is a semi-synthetic tetracycline antibiotic that serves as a potent inhibitor of hypoxia-inducible factor (HIF)-1α, demonstrating significant anti-inflammatory and neuroprotective properties. In addition to its bacteriostatic effects through binding to the 30S subunit of bacterial ribosomes, Minocycline reduces glutamate neurotransmission, contributing to its antidepressant effects. This compound is employed in research applications focused on cancer, neurodegenerative diseases, and the modulation of inflammatory responses. -
HIF-1α inhibitor
PRLX-93936 dihydrochloride (Compound 16) is a small-molecule inhibitor of hypoxia-inducible factor 1α (HIF-1α) with demonstrated anticancer activity. It also suppresses signaling within the activated Ras pathway, thereby inhibiting tumor cell proliferation and survival. PRLX-93936 shows potential therapeutic relevance in the study of relapsed or refractory multiple myeloma and other Ras-driven malignancies, making it a useful compound for investigating hypoxia-related and oncogenic signaling mechanisms in cancer. -
Hsp90/HSV inhibitor
AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research. -
p300/HIF-1α Inhibitor
KCN1 is an inhibitor of the p300/HIF-1α interaction. It functions by binding to the CH1 domain of p300, thereby disrupting the assembly of the p300/HIF-1α complex and inhibiting HIF transcriptional activity. KCN1 demonstrates significant antitumor properties, primarily through the induction of cell cycle arrest, making it a valuable tool for cancer research.
