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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
TrxR/EGFR Inhibitor
TrxR/EGFR-IN-1 is a potent inhibitor targeting both Thioredoxin Reductase (TrxR) and Epidermal Growth Factor Receptor (EGFR). This compound demonstrates significant anti-proliferative effects against Gefitinib-sensitive and resistant lung cancer cells, facilitating apoptosis and tumor cell death. TrxR/EGFR-IN-1 promotes GPX4 protein degradation via autophagolysosomal and proteasomal pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it a valuable tool for studying mechanisms underlying Gefitinib-resistant lung cancer. -
ErbB-2/EGFR Inhibitor
Lapatinib tosylate is a potent inhibitor targeting the ErbB-2 and EGFR tyrosine kinase domains. With IC50 values of 10.2 nM for EGFR and 9.8 nM for ErbB-2, it effectively blocks signaling pathways associated with cell proliferation and survival. This compound is primarily utilized in cancer research and therapeutic studies, particularly for conditions driven by aberrant ErbB signaling. -
VEGFR-2/DHFR Inhibitor
VEGFR-2/DHFR-IN-2 is a dual inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) and Dihydrofolate Reductase (DHFR), exhibiting IC50 values of 0.623 μM and 9.085 μM, respectively. This compound demonstrates significant cytotoxic activity against various cancer cell lines, including C26, HepG2, and MCF7, with IC50 values ranging from 3.59 to 8.38 μM. VEGFR-2/DHFR-IN-2 is pertinent for research applications focused on cancer therapeutics and targeted inhibition of tumor angiogenesis. -
VEGFR-2/DHFR Inhibitor
VEGFR-2/DHFR-IN-1 is a dual inhibitor of VEGFR-2 and dihydrofolate reductase (DHFR), exhibiting IC50 values of 0.384 μM and 7.881 μM, respectively. This compound demonstrates significant antibacterial activity against various strains, including Escherichia coli and MRSA, with MIC values ranging from 8 to 16 μg/mL. Additionally, VEGFR-2/DHFR-IN-1 shows potent cytotoxic effects on cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM. This reagent is applicable for research exploring cancer therapeutics and microbial resistance. -
Syk Inhibitor
Syk Inhibitor II is a highly selective, ATP-competitive inhibitor of spleen tyrosine kinase (Syk) with an IC50 of 41 nM. It effectively inhibits 5-hydroxytryptamine (5-HT) release from rat basophilic leukemia (RBL) cells, demonstrating an IC50 of 460 nM. This compound exhibits a lower potency against other kinases, making it a valuable tool for studying Syk-mediated signaling pathways and exploring its potential in anti-allergic research applications. -
Syk Inhibitor
Syk Inhibitor II dihydrochloride is a highly selective, ATP-competitive inhibitor of Spleen Tyrosine Kinase (Syk) with an IC50 of 41 nM. It effectively inhibits 5-HT release from rat basophilic leukemia (RBL) cells, demonstrating an IC50 of 460 nM. This compound exhibits reduced potency against other kinases, making it a valuable tool for research applications in immunology and allergy research, particularly in studies investigating Syk's role in signaling pathways associated with allergic responses. -
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. -
EGFR Inhibitor
Afatinib N-Oxide is an oxidative degradation product of Afatinib dimaleate, an irreversible inhibitor of the epidermal growth factor receptor (EGFR) family. This compound serves as a valuable tool for characterizing the stability and degradation pathways of Afatinib in chemical research. It may also aid in understanding the mechanistic effects of EGFR inhibition in various biological contexts. -
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-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-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. -
HIF-2α Inhibitor
HIF-2α-IN-14 is a selective inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α) with an IC50 value of 0.27 μM. This compound effectively disrupts HIF-2α signaling pathways, which are implicated in various pathological conditions, including cancer and ischemia. HIF-2α-IN-14 is useful in research settings aimed at elucidating the role of HIF-2α in cellular responses to hypoxia and in the development of potential therapeutic strategies targeting HIF-2α-mediated processes. -
HIF-2α Inhibitor
HIF-2α-IN-11 is a specific inhibitor of Hypoxia-Inducible Factor 2 alpha (HIF-2α), exhibiting an IC50 of 59.2 nM. This compound effectively disrupts HIF-2α activity, which is crucial in various biological processes, including cellular responses to hypoxia and tumorigenesis. Research applications include studies on cancer metabolism, angiogenesis, and the role of HIF-2α in pathological conditions associated with oxygen deficiency. -
HIF/HIF PHD Inhibitor
IOX2 sodium is a selective inhibitor of prolyl hydroxylase-2 (PHD2), with an IC50 of 22 nM. This compound effectively enhances HIF-1α expression while inhibiting reactive oxygen species (ROS) production, thereby influencing platelet function and arterial thrombosis. IOX2 sodium is applicable in research focused on thrombotic diseases and related mechanisms. -
HIF-PHD Inhibitor
HIF-PHD-IN-5 is an inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD) enzymes. This compound enhances the stability of hypoxia-inducible factors, leading to increased expression of target genes associated with cellular responses to low oxygen levels. HIF-PHD-IN-5 is primarily utilized in research focused on neurological diseases, providing insights into hypoxia-related pathophysiology and potential therapeutic interventions. -
HIF Inhibitor
CL67 is a potent inhibitor of the hypoxia-inducible factor (HIF) pathway. It interferes with G-quadruplex structures within promoter sequences, disrupting HIF-mediated transcriptional regulation. This compound is applicable in research related to renal cancer and studying the role of hypoxia in tumor progression. -
HIF/HIF Prolyl-Hydroxylase Inhibitor
HIV-IN-7 is a hypoxia-inducible factor (HIF) prolyl-hydroxylase inhibitor that modulates the stability and activity of HIF under normoxic conditions. This compound enhances the expression of hypoxia-responsive genes, making it a valuable tool for studying cellular response to low oxygen levels. HIV-IN-7 is pertinent in research applications related to cancer biology, ischemic diseases, and metabolic disorders. Its ability to influence cell differentiation and growth under hypoxic conditions further underscores its potential in therapeutic development. -
HIF-2α Inhibitor
HIF-2α-IN-15 is a selective inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α), demonstrating an IC50 value of 0.41 μM. This compound effectively disrupts HIF-2α signaling, which is crucial in processes such as cellular adaptation to hypoxia and cancer progression. HIF-2α-IN-15 is suitable for research applications focused on cancer biology, ischemia, and other diseases where HIF-2α plays a significant role in disease pathology. -
HIF-PHD Inhibitor
DS44470011 is a potent inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PHD). This compound exhibits oral bioactivity and is known to enhance the release of erythropoietin (EPO) from cells. DS44470011 is suitable for research applications focused on renal anemia and the regulation of erythropoiesis under hypoxic conditions. -
HIF Hydroxylase Inhibitor
TRC160334 is a potent inhibitor of hypoxia-inducible factor (HIF) hydroxylases. This compound primarily enhances HIF stabilization, making it a valuable tool in studies related to ischemia/reperfusion injury and other hypoxic conditions. Its mechanism of action enables researchers to investigate the role of HIF in cellular responses to oxygen deprivation and identify potential therapeutic avenues for related pathologies. -
HIF-1α/CBR1 Inhibitor
5,3',4',3'',4'',5''-6-O-Ethyl-EGCG is a selective inhibitor of HIF-1α and CBR1. This compound effectively reduces the expression levels of HIF-1α and CBR1 at both mRNA and protein levels, making it a valuable tool for investigating hypoxia-related pathways and metabolic regulation. Its optimized structure enhances its potency as an adjuvant in various chemical research applications focused on cellular response to hypoxia. -
HIF-1α-p300/CBP Inhibitor
KST012174 hydrochloride is a selective inhibitor of the HIF-1α-p300/CBP interaction, demonstrating an IC50 of 107 μM. It effectively disrupts the binding of HIF-1α to the p300 protein at concentrations of 100 μM without altering HIF-1α protein stability. By targeting the C-terminal transactivation domain of HIF-1α and the CH1 domain of p300, KST012174 hydrochloride inhibits HIF-1α-mediated transcriptional activation, leading to decreased VEGF mRNA expression and suppression of tumor angiogenesis. This reagent is valuable for research into cancer biology and hypoxia-related pathways. -
HIF Hydroxylase Inhibitor
TRC160334 sodium is an inhibitor of hypoxia-inducible factor (HIF) hydroxylase. This compound effectively stabilizes HIF under normoxic conditions, promoting cellular responses to low oxygen levels. TRC160334 sodium is primarily utilized in research related to ischemia/reperfusion injury and other conditions involving hypoxia. -
HIF-2α Inhibitor
HIF-2α-IN-13 is a selective inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α), exhibiting an IC50 value of 2.7 μM. This compound disrupts HIF-2α activity, influencing cellular responses to hypoxia. HIF-2α-IN-13 is valuable for research applications in understanding cancer biology, metabolism, and related signaling pathways. -
HIF-1α Inhibitor
HIF-1α-IN-10 is a small molecule inhibitor targeting Hypoxia-Inducible Factor 1-alpha (HIF-1α). This compound serves as a ligand for the synthesis of PROTAC molecules, enabling the development of HIF-1α degraders such as PROTAC HIF-1α degrader-2. It is primarily utilized in research investigating hypoxia-related pathways and cancer biology, offering potential insights into therapeutic strategies for diseases associated with HIF-1α dysregulation.
