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. - Oroxylin A is an O-methylated flavone, It has demonstrated activity as a dopamine reuptake inhibitor and is also a negative allosteric modulator of the benzodiazepine site of the GABAA receptor.
- Paramesha Bugga, .et al. , Cell Signal, 2022, Jun;94:110309 PMID: 35304284
- Bugga Paramesha, .et al. , Antioxidants (Basel), 2021, Feb 24;10(3):338 PMID: 33668369
- Mai Nagasaka, .et al. , Molecules, 2018, Jun; 23(6): 1394 PMID: 29890668
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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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Apoptotic, antiproliferative and antiangiogenic agent
2-Methoxyestradiol is an apoptotic, antiproliferative and antiangiogenic agent. Induces p53-induced apoptosis via two pathways: activation of p38 and NF-κB; and activation of JNK and AP-1 leading to Bcl-2 phosphorylation. - Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).
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Smad3/HIF-α Dual Target PROTAC
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine functions as a dual-target PROTAC, effectively inducing ubiquitination and degradation of Smad3 while simultaneously enhancing HIF-α protein levels. This compound exhibits multi-pathway anti-fibrotic activity and renal protective properties, making it valuable for research on renal anemia. Additionally, it has potential applications in studying prostate cancer and other malignancies, contributing to a deeper understanding of cancer biology and treatment modalities. -
Iron Chelator
Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19. -
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. -
PROTAC HIF-1α Degrader
PROTAC HIF-1α Degrader-2 is a selective degrader that targets HIF-1α, facilitating its degradation through the ubiquitin-proteasome pathway by promoting the formation of a HIF-1α/VHL ternary complex. This compound has been shown to inhibit the proliferation, migration, and colony formation of HeLa cells while also inducing apoptosis. Moreover, PROTAC HIF-1α Degrader-2 decreases the expression of p-MEK and p-AKT within the MAPK and PI3K/AKT signaling pathways, making it a valuable tool for research into cervical cancer. -
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. -
HIF-1α/EZH2 Inhibitor
DYB-03 is an orally active inhibitor of HIF-1α and EZH2. It effectively suppresses migration, invasion, and angiogenesis in lung cancer cells as well as human umbilical vein endothelial cells (HUVECs), demonstrated both in vitro and in vivo. Additionally, DYB-03 induces apoptosis in A549 and H460 cells that are resistant to 2-ME2 and GSK126, highlighting its potential in overcoming resistance in lung cancer therapies. -
HIF1-α Inhibitor
Oltipraz metabolite M2 is an active metabolite that serves as a HIF-1α inhibitor. It enhances mitochondrial fuel oxidation and inhibits lipogenesis in the liver by activating AMPK, particularly in high-fat diet-fed mouse models. This compound is valuable for research focused on hepatic steatosis and steatohepatitis. -
HIF-1α Inhibitor
LW1564 is a potent inhibitor of HIF-1α, demonstrating an IC50 of 1.2 µM in HepG2 cells. It disrupts mitochondrial respiration, decreases ATP production, promotes HIF-1α degradation, and inhibits the proliferation of diverse cancer cell types with a GI50 ranging from 0.4 to 4.6 μM. Additionally, LW1564 activates the AMPK signaling pathway while inhibiting lipid synthesis, showcasing its potential for research in cancer biology. Its antitumor efficacy has also been validated in a HepG2 xenograft mouse model. -
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. -
interferon inducer
Tilorone Dihydrochloride is an antiviral, antineoplastic, and anti-inflammatory agent; Orally active interferon inducer, inhibiting Ebola virus (EBOV). -
iron chelator
Deferoxamine mesylate is an iron chelator that binds free iron in a stable complex, preventing it from engaging in chemical reactions. - Amifostine is a phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.
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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.
