Catalog No.
Product Name
Application
Product Information
Citations
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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-2α Agonist
ZG-2686 is a selective HIF-2α agonist that exhibits potent activity with an EC50 of 0.25 µM. By binding to a distinct internal cavity of HIF-2α, it stabilizes the HIF-2α/β heterodimer through hydrogen bonds with structural water molecules, thereby enhancing transcriptional activity. This compound has demonstrated the capability to synergize with Vadadustat to upregulate HIF-2α-dependent EPO gene expression in both in vitro and in vivo models. ZG-2686 is valuable for research focusing on renal anemia mechanisms and potential therapeutic approaches. -
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. -
HIF-1α Inhibitor
CHNQD-03301 is a potent orally active inhibitor of hypoxia-inducible factor-1 alpha (HIF-1α) with an IC50 value of 10.97 nM. This compound induces proteasomal degradation of HIF-1α, effectively suppressing its accumulation. CHNQD-03301 has demonstrated the ability to reverse angiogenesis induced by HIF accumulation and reduce the HIF-driven erythrocytosis phenotype in zebrafish models. It is a valuable tool for investigating HIF-1α-related processes in colon cancer research. -
HIF/HIF Prolyl-Hydroxylase
HIF-1/2α-IN-3 is a selective inhibitor of the hypoxia-inducible factor 1 and 2 alpha (HIF-1α and HIF-2α), targeting prolyl hydroxylase enzymes. This compound plays a critical role in modulating hypoxic response pathways by inhibiting HIF stabilization and activity. HIF-1/2α-IN-3 is useful in research applications focused on cancer biology, angiogenesis, and metabolic disorders, wherein HIF signaling plays a significant role in cellular adaptation to low oxygen conditions. -
HIF1α CTAD Analog
OHM1 is an analog of the HIF1α C-terminal transactivation domain (CTAD) that selectively inhibits the interaction between HIF1α and the coactivators p300/CBP. With an affinity of 0.53 μM for the CH1 domain, OHM1 effectively disrupts HIF1α-mediated transcriptional activity. This compound is valuable for research applications focused on hypoxia signaling, cancer biology, and the regulation of cellular responses to oxygen levels. -
HIF-2α Inhibitor
HIF-2α-IN-12 is a selective inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α), exhibiting an IC50 value of 0.9 μM. This compound plays a crucial role in research focused on cancer biology and ischemic conditions by modulating the HIF-2α pathway. Its ability to inhibit HIF-2α makes it a valuable tool for studying cellular responses to hypoxia and evaluating potential therapeutic strategies. -
HIF-PHD2 Inhibitor
DS79540454 is a selective inhibitor of hypoxia-inducible factor prolyl hydroxylase domain 2 (HIF-PHD2) with an IC50 of 0.26 μM. This compound plays a crucial role in regulating cellular responses to hypoxia by stabilizing hypoxia-inducible factor (HIF) levels. DS79540454 is primarily utilized in studies related to renal anemia and offers insights into the therapeutic modulation of erythropoiesis under hypoxic conditions. -
HIF-2α Inhibitor
HIF-2α-IN-10 is a potent inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α), demonstrating an IC50 value of 0.05 μM. This compound effectively disrupts the HIF-2α signaling pathway, which is known to play a critical role in tumorigenesis and cancer progression. HIF-2α-IN-10 is primarily utilized in research focused on cancer biology, providing insights into therapeutic interventions targeting hypoxic conditions. -
HIF Inhibitor
Arylsulfonamide 64B is a potent inhibitor of hypoxia-inducible factor (HIF). This compound effectively suppresses hypoxia/HIF-mediated expression of key oncogenes such as c-Met and CXCR4, thereby demonstrating significant anti-tumor activity. Arylsulfonamide 64B is particularly relevant for research focused on uveal melanoma, as it has been shown to reduce primary tumor growth and metastasis in mouse models. -
HIF-2α Inhibitor
HIF-2α-IN-16 is a selective inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α), exhibiting an IC50 of 0.091 μM. This compound demonstrates significant biological activity by interfering with HIF-2α signaling pathways, which are implicated in various cancerous conditions and other hypoxic responses. HIF-2α-IN-16 is commonly utilized in research to investigate its effects on tumor growth, metabolism, and related therapeutic approaches. -
HIF-2α Inhibitor
HIF-2α-IN-5 is a potent inhibitor of HIF-2α, demonstrating an IC50 of less than 50 nM. This compound effectively disrupts the hypoxia-inducible factor signaling pathway, making it a valuable tool for studying cellular responses to low oxygen conditions. HIF-2α-IN-5 has potential applications in cancer research and other fields where hypoxia plays a critical role in disease progression. -
HIF-1α Inhibitor
HIF-1α-IN-7 is a potent inhibitor of hypoxia-inducible factor 1-alpha (HIF-1α), a key regulator of cellular responses to hypoxia. This compound exhibits neuroprotective activity and has potential applications in Alzheimer's disease research, enabling investigations into mechanisms of neurodegeneration and hypoxic responses in neuronal cells. -
HIF-2α Inhibitor
HIF-2α-IN-9 is a selective inhibitor of HIF-2α, effectively modulating hypoxia-responsive pathways. This compound demonstrates significant inhibition of VEGF-A with an IC50 value of 305 nM, influencing tumor growth and angiogenesis. HIF-2α-IN-9 also promotes reactivation of macrophage-mediated tumor immunity, making it a valuable tool for research in cancer biology and therapeutic approaches targeting tumor microenvironments. -
HIF Inhibitor
CLB-016 is a potent inhibitor of Hypoxia-inducible factor 1 (HIF-1) with an IC50 of 19.1 µM. This compound effectively suppresses HIF-1-mediated responses to hypoxia, making it a valuable tool for research focused on cellular adaptation to low oxygen conditions. CLB-016 is applicable in studies examining the role of HIF in tumor progression, metabolic regulation, and other hypoxia-related pathologies. -
HIF/HIF Prolyl-Hydroxylase
EZN-2968 is an antisense oligonucleotide designed to selectively bind and inhibit the expression of HIF-1α mRNA, targeting the hypoxia-inducible factor (HIF) pathway. By reducing HIF-1α levels, EZN-2968 demonstrates significant anti-tumor activity, effectively suppressing tumor cell proliferation. This reagent is valuable for research applications focused on cancer biology and therapeutic strategies targeting the hypoxic response in tumors. -
HIF Activator
ML228 analog serves as a potent activator of hypoxia-inducible factor (HIF), a critical regulator of cellular responses to hypoxic stress. This compound is utilized in research to study HIF-related pathways and its implications in various physiological and pathological conditions, including cancer and metabolic disorders. Its ability to enhance HIF activity makes it a valuable tool for exploring therapeutic strategies targeting hypoxia-responsive mechanisms. -
HIF-2α Agonist
ZG-2033 is a potent orally active HIF-2α agonist, exhibiting an EC50 value of 490 nM in luciferase reporter gene assays. This compound has been shown to alleviate anemia and operates synergistically with AKB-6548 in enhancing erythropoiesis. ZG-2033 serves as a valuable tool for research focused on renal anemia and related therapeutic interventions. -
ErbB-2/EGFR Tyrosine Kinase Inhibitor
GW583340 is an orally bioavailable inhibitor targeting the ErbB-2 and EGFR tyrosine kinases. It demonstrates significant antitumor activity in xenograft models characterized by overexpression of EGFR or ErbB-2, making it a valuable tool for investigating therapeutic strategies. GW583340 is particularly relevant for research focused on head and neck cancer, breast cancer, and gastric cancer. -
EGFR PARP Dual-targeting PROTAC Molecule
DP-C-4 is a Cereblon-based dual-targeting PROTAC molecule designed for the concurrent degradation of epidermal growth factor receptor (EGFR) and poly (ADP-ribose) polymerase (PARP). This compound demonstrates significant biological activity by promoting the targeted destruction of these proteins, which can be crucial in cancer research and therapeutic applications. DP-C-4 may facilitate studies investigating the interplay between EGFR and PARP pathways, potentially leading to new insights in oncology and the development of innovative treatment strategies. -
PROTAC BCR-ABL Degrader
SNIPER(ABL)-020 is a PROTAC compound designed to selectively degrade the BCR-ABL fusion protein through targeted ubiquitin-proteasome pathway engagement. By conjugating Dasatinib, an ABL inhibitor, with Bestatin, an IAP ligand, SNIPER(ABL)-020 effectively promotes the protein's ubiquitination and subsequent degradation. This reagent is valuable for research focused on chronic myeloid leukemia and BCR-ABL related signaling pathways, offering insights into targeted protein degradation mechanisms in cancer therapeutics. -
EGFR T790M/L858R/ACK1 Inhibitor
EGFR/ACK1-IN-1 is a potent inhibitor targeting the EGFR T790M/L858R mutation and ACK1, with IC50 values of 23 nM and 263 nM, respectively. This dual inhibition effectively disrupts cell proliferation and demonstrates significant antitumor activity. It is a valuable reagent for research applications focused on cancer biology and therapeutic development for EGFR mutant-driven tumors. -
ALK Degrader
ALK-IN-35 is an ALK degrader that selectively inhibits ALK kinase activity with an IC50 of 0.74 nM. This compound increases the solvent-accessible surface area of hydrophobic residues around the ALK binding pocket, leading to a partially unfolded conformation that promotes proteasomal degradation of ALK. ALK-IN-35 has demonstrated potent anti-proliferative effects on cancer cells and is a valuable tool for research focused on non-small cell lung cancer. -
EphB4, VEGFR-2 and PDGFR-β Inhibitor
JI-101 hydrochloride is an orally active inhibitor targeting EphB4, VEGFR-2, and PDGFR-β, effectively modulating angiogenesis signaling pathways associated with tumor vasculature. This compound demonstrates significant anti-cancer activity, inhibiting multiple stages of tumor angiogenesis and showing efficacy against various cancer cell lines and xenografts. With rapid oral absorption and extensive tissue distribution, preferential uptake occurs in the lungs, while elimination primarily occurs via feces. JI-101 hydrochloride can be utilized in research studies focused on ovarian cancer and other solid tumors, providing valuable insights into angiogenesis and cancer treatment mechanisms. -
ALK4/5/7 Inhibitor
A 83-01 sodium is a selective inhibitor of the transforming growth factor-beta (TGF-β) type I receptors ALK4, ALK5, and ALK7. With IC50 values of 12 nM, 45 nM, and 7.5 nM, it effectively blocks transcriptional activity induced by these kinases. This compound is valuable for research applications focused on TGF-β signaling pathways and regulation of cellular processes such as proliferation, differentiation, and epithelial-mesenchymal transition. -
ALK2 Inhibitor
M4K-2009 is a potent inhibitor of ALK2, exhibiting an IC50 value of 13 nM, and is capable of penetrating the blood-brain barrier. In addition to its primary activity against ALK2, M4K-2009 demonstrates efficacy against the hERG potassium channel. This compound is valuable for research in the areas of bone morphogenetic protein signaling and related therapeutic applications. -
Chiral Shift Reagent
(R)-(-)-1-(9-Anthryl)-2,2,2-trifluoroethanol serves as a chiral shift reagent, facilitating the determination of enantiomeric ratios in various compounds. Its primary application lies in nuclear magnetic resonance (NMR) spectroscopy, where it aids in assessing optical purity. This reagent is essential for researchers aiming to quantify chirality and enhance the understanding of stereochemical properties in synthetic and natural products. -
AKT1/SRC/STAT3/EGFR Binder
(+)−Theta-cypermethrin is a stereoisomer of cypermethrin that functions as a selective binder to AKT1, SRC, STAT3, and epidermal growth factor receptor (EGFR). This compound is known to penetrate the blood-brain barrier, leading to alterations in the amplitude of delayed rectifier potassium channel currents and significant shifts in the activation and inactivation curves at elevated concentrations. Additionally, (+)-Theta-cypermethrin induces abnormal electrical activity in rat hippocampal neurons and is associated with chronic respiratory system damage and neurotoxicity. It serves as a valuable tool for research into signal transduction pathways and neuropharmacology. -
HIF/HIF Prolyl-Hydroxylase
(Rac)-Dencichine, the racemic form of Dencichin, targets Hypoxia-Inducible Factor (HIF) by inhibiting HIF prolyl-hydroxylase-2 (PHD-2) activity. This non-protein amino acid, derived from Panax notoginseng, exhibits significant biological activity in promoting HIF stabilization under normoxic conditions. Its ability to modulate HIF pathways makes it valuable in research applications related to cancer biology, ischemia, and metabolic regulation. -
ALK Molecular Glue Degrader
TRI-611 is an orally active molecular glue degrader that targets the anaplastic lymphoma kinase (ALK). It forms a ternary complex with the substrate receptor CRBN, leading to polyubiquitination and subsequent degradation of ALK, including resistant fusion proteins. TRI-611 effectively inhibits ALK-mediated downstream signaling and exhibits anti-proliferative effects in ALK-positive cancer cells. Preclinical studies demonstrate its capability to induce regression of ALK-positive non-small cell lung cancer tumors, making it a valuable tool for research into TKI-refractory tumors and central nervous system metastases. -
EGFR Ligand
Cyclo[K(N3)larllt] is a cyclic peptide that specifically targets the epidermal growth factor receptor (EGFR) with a Kd value of 5.09 μM and demonstrates selectivity for related proteins HER2 and HER3. This compound exhibits no cytotoxicity and does not inhibit the growth of EGFR-overexpressing cancer cells. Cyclo[K(N3)larllt] is ideal for use as a ligand in EGFR-targeted fluorescent conjugates, facilitating the detection of tumors with elevated EGFR levels. Its applications extend to research focused on colorectal cancer and related pathologies. -
VEGFR Ligand
Peptide HRH is a polypeptide that specifically targets vascular endothelial growth factor receptors (VEGFR). It effectively inhibits VEGF-stimulated endothelial cell proliferation, thereby disrupting angiogenesis. Additionally, Peptide HRH demonstrates efficacy in suppressing corneal neovascularization. This peptide is suitable for research applications focused on anti-angiogenesis and related studies. -
VEGFR2 Inhibitor
VEGFR2-IN-84 is a potent VEGFR2 inhibitor that operates as a multi-targeted tyrosine kinase inhibitor utilizing a naphthalene ring scaffold. It exhibits sub-nanomolar affinity for VEGFR2 and effectively inhibits other kinases, including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 disrupts the phosphorylation of VEGFR2, leading to significant reduction in endothelial cell proliferation, migration, and tumor angiogenesis. This compound demonstrates broad antiproliferative activity against various solid tumors, such as liver, lung, and renal cancers, while exhibiting low toxicity to normal cells. VEGFR2-IN-84 is suitable for research applications focused on malignant tumors. -
EGFR Inhibitor
ZW-49 is a potent orally active pan-EGFR inhibitor, demonstrating IC50 values ranging from 0.03 to 1.5 nM. This compound selectively targets various EGFR mutations while sparing wild-type EGFR and other familial targets, effectively blocking the ATP-binding pocket and a conserved hydrophobic subpocket without causing steric conflicts with PACC mutation P loops. ZW-49 exhibits significant anti-proliferative activity by inhibiting cancer cell proliferation, inducing G0/G1 phase cell-cycle arrest, and promoting apoptosis, making it a valuable reagent for cancer research, particularly in non-small cell lung cancer models. -
EGFR Inhibitor
Rinumafusp alfa is a human monoclonal antibody that specifically inhibits the epidermal growth factor receptor (EGFR) by targeting ERBB3/HER3. This compound demonstrates potential in blocking tumor cell signaling pathways, thereby impeding tumor growth and progression. It is primarily utilized in research applications focused on cancer biology and therapeutic development targeting EGFR-related pathways. -
FLT3 Inhibitor
FLT3-IN-40 is a type I ATP-competitive inhibitor of FLT3, demonstrating an IC50 of 16.26 nM. This compound effectively reduces FLT3 autophosphorylation and downregulates ERK phosphorylation, thereby exhibiting significant antiproliferative activity, influencing cell cycle regulation, and promoting apoptosis. FLT3-IN-40 is particularly valuable for research applications focused on acute myeloid leukemia. -
VEGFR/Tyrosine Kinase Src Inhibitor
TG 100948 is a dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and tyrosine kinase Src. This compound demonstrates significant biological activity by reducing retinal edema and retinal thickening, as well as eliminating bullous edema cysts in rat models of ischemic retinal vein occlusion. TG 100948 is valuable for research into the pathophysiology and potential treatments of ischemic retinal vein occlusion.
