Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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/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
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. -
VEGF/HIF-1 Inducer
Mersalyl is a potent inducer of vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1). It enhances the expression of VEGF and ENO1 mRNA, contributing to its biological activity. Mersalyl is utilized in research to investigate mechanisms underlying hypoxia and angiogenesis, as well as potential therapeutic effects related to diuresis. -
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. -
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. -
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. -
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. -
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. -
HIF2α siRNA
Zifcasiran sodium is a synthetic double-stranded siRNA designed to target hypoxia-inducible factor-2α (HIF2α), modulating its expression and disrupting pro-oncogenic signaling pathways. This reagent effectively engages the RNA interference (RNAi) machinery, facilitating the degradation of HIF2α (EPAS1) mRNA, which leads to a decrease in translated HIF2α protein levels. Zifcasiran sodium is particularly relevant in research focused on clear cell renal cell carcinoma (ccRCC) and the mechanisms of tumor growth regulation. -
HIF-2 Agonist
M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist that enhances the expression of HIF-2 target genes. This compound exhibits synergistic effects when used in conjunction with prolyl-hydroxylase domain (PHD) inhibitors, making it a valuable tool for research into hypoxic conditions and related pathways. Its potential applications span across studies in cancer biology, metabolism, and various physiological responses to low oxygen levels. -
HIF/HIF Prolyl-Hydroxylase Inhibitor
Naphthofluorescein is a potent inhibitor of HIF-1 through the inhibition of HIF prolyl-hydroxylase activity. It effectively suppresses Mint3-dependent HIF-1 signaling and glycolytic activity in cancer cells and macrophages while exhibiting low cytotoxicity in vitro and negligible adverse effects in vivo. Additionally, Naphthofluorescein serves as a fluorescent pH-sensitive probe, making it suitable for functional Cerenkov imaging applications. -
HIF/HIF Prolyl-Hydroxylase Inhibitor
Dencichine is a non-protein amino acid derived from Panax notoginseng, primarily functioning as an inhibitor of hypoxia-inducible factor prolyl-hydroxylase-2 (PHD-2). By inhibiting PHD-2 activity, Dencichine enhances the stability and accumulation of hypoxia-inducible factors, which play a crucial role in cellular responses to low oxygen conditions. This compound is significant for research applications related to hypoxia, angiogenesis, and cancer therapy. -
HIF-1α Inhibitor
HIF-1α-IN-2 is a potent inhibitor of HIF-1α, demonstrating significant anticancer activity with IC50 values of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cell lines, respectively. This compound functions by inhibiting the transcription and translation of HIF-1α, effectively suppressing its expression. HIF-1α-IN-2 is applicable in research exploring hypoxia-induced tumor progression and therapeutic resistance in cancer studies. -
HIF-1α Inhibitor
Dimethyl-bisphenol A (DMBPA) is a potent inhibitor of the hypoxia-inducible factor 1-alpha (HIF-1α). By effectively reducing Vegfa mRNA expression, DMBPA plays a significant role in the regulation of angiogenesis and tumor growth. This compound is valuable for research focusing on cancer biology, hypoxia signaling pathways, and therapeutic strategies targeting HIF-1α. -
HIF-1 Inhibitor
HIF-1 inhibitor-4 is a potent HIF-1 inhibitor with an IC50 value of 560 nM. This compound effectively decreases the protein levels of HIF-1α without influencing its mRNA expression. HIF-1 inhibitor-4 is intended for research applications focused on hypoxia signaling pathways and the modulation of tumor microenvironments. -
HIF-2α Stabilizer
AKB-6899 is a selective HIF-2α stabilizer that functions as a prolyl hydroxylase domain 3 (PHD3) inhibitor. This compound enhances the production of the soluble form of the VEGF receptor (sVEGFR-1) in GM-CSF-treated macrophages. AKB-6899 exhibits notable antitumor and antiangiogenic properties, making it valuable for research applications focused on cancer biology and vascular biology. -
HIF-2α Agonist
HIF-2α Agonist 2 is a selective activator of hypoxia-inducible factor 2 alpha (HIF-2α), exhibiting an EC50 value of 1.68 μM at a concentration of 20 μM. This compound demonstrates non-cytotoxicity in 786-O-HRE-Luc cells, making it suitable for various in vitro studies. HIF-2α Agonist 2 is an important tool for researching oxygen metabolism and related pathways in cellular response to hypoxic conditions. -
HIF-1 Inhibitor
HIF-IN-1 is a selective inhibitor of hypoxia-inducible factor-1 (HIF-1), effectively reducing HIF-1α protein levels without altering HIF-1α mRNA expression. This compound exhibits minimal cytotoxicity, making it suitable for studies requiring modulation of hypoxic responses. HIF-IN-1 is valuable in cancer research and other areas investigating the role of HIF-1 in cellular adaptation to low oxygen conditions. -
HIF-PHD Inhibitor
GSK360A is a potent and orally bioavailable inhibitor of hypoxia-inducible factor prolyl hydroxylases (HIF-PHD) with IC50 values of 10 nM, 100 nM, and 126 nM for PHD1, PHD2, and PHD3, respectively. This compound effectively activates the HIF-1 alpha signaling pathway, providing protective effects on the heart in the context of myocardial infarction (MI). GSK360A holds potential for advancing therapeutic strategies in cardiovascular research and conditions related to oxygen deprivation. -
HIF-1α/β Inhibitor
KG-548 is a potent HIF-1α/β inhibitor that disrupts the ARNT/TACC3 complex formation by competitively binding to the ARNT PAS-B domain. By inhibiting the interaction between ARNT (aryl hydrocarbon receptor nuclear translocator) and TACC3, KG-548 plays a crucial role in modulating hypoxia-inducible factor pathways. This compound is valuable for research applications focused on cancer biology, metabolism, and hypoxic tumor microenvironments. -
HIF1 Inhibitor
HIF1 agonist-1 is a potent activator of Hypoxia-Inducible Factor 1 (HIF1) with an EC50 value of 0.9 μM. This compound enhances HIF1 activity, promoting various cellular responses to hypoxic conditions. It serves as a valuable tool for research into cancer biology and potential therapeutic strategies targeting tumor microenvironments. -
HIF-1α/DLL4 Inhibitor
Steppogenin is a selective inhibitor of HIF-1α and DLL4, exhibiting IC50 values of 0.56 μM and 8.46 μM, respectively. This compound demonstrates significant biological activity in modulating angiogenesis and can be utilized in research focusing on angiogenic diseases, particularly those associated with solid tumors. Its inhibitory properties make it a valuable tool for investigating the underlying mechanisms of tumor pathogenesis and vascularization. -
HIF-1/2α Inhibitor
HIF-1/2α-IN-2 is a selective inhibitor of hypoxia-inducible factors HIF-1 and HIF-2α, effectively reducing their levels in biological systems. This compound triggers an iron starvation response by specifically targeting Iron Sulfur Cluster Assembly 2 (ISCA2). HIF-1/2α-IN-2 is utilized in research focused on tumor biology, ischemia, and metabolic disorders, contributing to a deeper understanding of cellular responses to hypoxia and iron dynamics. -
HIF2α Inhibitor
NVP-DFF332 is a potent HIF2α inhibitor that demonstrates inhibitory activity with IC50 values of 9 nM for HIF2α SPA, 37 nM for HIF2α iScript, and 246 nM for HIF2α HRE RGA. This compound exhibits significant antitumor effects, making it valuable for cancer research focused on hypoxia-inducible factors. Its ability to modulate HIF2α activity positions NVP-DFF332 as a promising tool for studying tumor biology and therapeutic interventions. -
HIF-1α Inhibitor
HIF-1α-IN-5 is a potent inhibitor of HIF-1α, exhibiting an IC50 of 24 nM in HEK293T cells. It also demonstrates inhibitory activity against MAO-A, contributing to its physiological effects. HIF-1α-IN-5 is effective in downregulating mRNA expressions of VEGF and PDK1 under hypoxic conditions, making it a valuable tool for cancer research. Its ability to modulate hypoxia-related pathways provides insights into tumor biology and potential therapeutic strategies. -
VHL:HIF-α Interaction Inhibitor
cis VH-298 is a VHL:HIF-α interaction inhibitor that disrupts the binding of hydroxylated HIF-1α peptides to the VHL complex. This compound demonstrates a significant loss of binding specificity, making it a valuable tool for investigating the hypoxia response pathway. Its applications extend to studies in cancer research, where modulation of HIF signaling is critical. -
HIF-1α Inhibitor
HIF-1α-IN-4 is an inhibitor of HIF-1α with an IC50 value of 24 nM in HEK293T cells. It effectively downregulates the expression of VEGF and PDK1 mRNA under hypoxic conditions. This compound is applicable in cancer research, particularly in studies focusing on the hypoxic tumor microenvironment and angiogenesis regulation. -
HIF-PHD Inhibitor
HIF-PHD-IN-1 is a potent inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), demonstrating an IC50 of 54 nM specifically for human HIF-PHD2. This compound exhibits significant biological activity by stabilizing hypoxia-inducible factors, thereby enhancing erythropoiesis. HIF-PHD-IN-1 holds potential for research applications in renal anemia therapy and related studies exploring oxygen-sensing pathways. -
HIF-2α Inhibitor
HIF-2α-IN-2 is a selective inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α), demonstrating an IC50 of 16 nM in scintillation proximity assays (SPA). This compound serves as a valuable tool for investigating the role of HIF-2α in various biological processes, including tumor hypoxia and angiogenesis. HIF-2α-IN-2 is suitable for research applications focusing on cancer biology and the modulation of hypoxic responses. -
HIF-2α Inhibitor
Davotifan is a bicyclic compound that functions as a potent inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α). It is primarily utilized in research focused on HIF-2α-related cancers, where it plays a critical role in tumor growth and progression. This compound enables the exploration of HIF-2α signaling pathways and their implications in cancer biology, facilitating the development of targeted therapeutic strategies. -
HIF-2α Inhibitor
HIF-2α-IN-3 is an allosteric inhibitor of hypoxia-inducible factor 2α (HIF-2α) that demonstrates an IC50 value of 0.4 µM and a KD of 1.1 µM. This compound has potential applications in cancer research due to its capacity to disrupt HIF-2α activity, which is implicated in tumorigenesis and adaptation to hypoxic conditions. It serves as a valuable tool for investigating the role of HIF-2α in cellular processes and therapeutic targets in oncology. -
HIF/HIF Prolyl-Hydroxylase Modulator
Acetylarenobufagin is a steroidal modulator of hypoxia-inducible factor 1 (HIF-1), primarily targeting HIF prolyl-hydroxylase. This compound exhibits significant biological activity through the regulation of HIF-mediated responses under hypoxic conditions. It is valuable for research applications focused on cancer biology, ischemia, and metabolic disorders where HIF signaling plays a critical role. -
HIF2α siRNA
Zifcasiran is a synthetic double-stranded siRNA designed to target hypoxia-inducible factor-2 alpha (HIF2α). By engaging the RNA interference (RNAi) pathway, Zifcasiran effectively degrades HIF2α mRNA, thereby inhibiting the expression of this key oncogenic factor in clear cell renal cell carcinoma (ccRCC). This mechanism reduces downstream pro-oncogenic signaling, making Zifcasiran a valuable tool for research on ccRCC and potential therapeutic applications in targeting hypoxia-related pathways. -
HIF-2α Inhibitor
HIF-1/2α-IN-1 is a potent inhibitor of HIF-2α, exhibiting an IC50 value of 0.92 μM. This compound also reduces HIF-1α levels, highlighting its potential to modulate hypoxic signaling pathways. HIF-1/2α-IN-1 is primarily utilized in research focused on clear cell renal cell carcinoma (ccRCC) and other related hypoxia-driven cancers, offering insights into therapeutic interventions targeting the HIF pathway. -
HIF-2α Inhibitor
Imdatifan is a potent inhibitor of hypoxia-inducible factor 2α (HIF-2α), demonstrating an EC50 value of 6 nM. This compound effectively modulates HIF-2α activity, making it a valuable tool for investigating various pathological conditions, including cancer, liver disease, inflammatory disorders, pulmonary diseases, and iron overload syndromes. Researchers may utilize Imdatifan to explore the role of HIF-2α in disease progression and therapeutic interventions. -
HIF/HIF Prolyl-Hydroxylase Inhibitor
Enarodustat hydrochloride is a potent inhibitor of hypoxia-inducible factor (HIF) and HIF prolyl-hydroxylase, exhibiting an EC50 of 0.22 μM. This compound is primarily investigated for its potential in the treatment of renal anemia by stabilizing HIF, thereby promoting erythropoiesis and improving oxygenation in tissues. It serves as a valuable tool for research in hypoxia-related pathways and anemia therapies. -
HIF-2α Inhibitor
HIF-2α-IN-6 is a selective inhibitor of the hypoxia-inducible factor 2-alpha (HIF-2α), a key regulator of cellular response to low oxygen levels. This compound effectively disrupts HIF-2α signaling, leading to reduced expression of downstream genes involved in angiogenesis, metabolism, and tumor progression. HIF-2α-IN-6 is commonly utilized in cancer research and studies investigating the role of hypoxia in various diseases, making it a valuable tool for understanding tumor microenvironments and developing potential therapeutic strategies. -
HIF2α Inhibitor
RH01504 is a potent inhibitor of HIF2α, exhibiting a Kd value of 5.42 nM against human HIF2α. This compound effectively suppresses the proliferation of renal cancer cells, making it a valuable tool for investigating renal cell carcinoma. RH01504 is applicable in research exploring the molecular mechanisms underlying hypoxia-driven tumor progression and offers potential insights into therapeutic strategies targeting HIF2α in cancer treatments. -
HIF-1 Inhibitor
103D5R is a potent inhibitor of hypoxia-inducible factor-1 (HIF-1) activation, exhibiting an IC50 of 35 µM through the suppression of HIF-1α protein synthesis. This compound also inhibits the proliferation of LN229 cells, with an IC50 of 26 µM, making it a valuable tool for research into tumor biology and the molecular mechanisms of hypoxia. Its applications extend to studies exploring the role of HIF-1 in cancer progression and therapy resistance. -
HIF-1α Inhibitor
HIF-1α-IN-3 is a hypoxia-selective inhibitor of HIF-1α, effectively disrupting its pathway under low oxygen conditions. This compound demonstrates significant antiestrogenic activity, making it a valuable tool for research in cancer biology and the study of hypoxic responses. Its selective inhibition of HIF-1α positions it for use in investigations related to tumor metabolism and therapeutic resistance.
