Catalog No.
Product Name
Application
Product Information
Citations
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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-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. -
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. -
HER2 Inhibitor
JBJ-08-178-01 is a selective tyrosine kinase inhibitor targeting mutant forms of the human epidermal growth factor receptor 2 (HER2). It demonstrates significant antitumor activity by reducing both the kinase activity and protein levels of HER2 through the induction of proteasomal degradation. This compound holds potential for research applications in non-small-cell lung cancer, providing insights into therapeutic mechanisms against HER2-driven malignancies. -
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. -
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. -
ALK Inhibitor
TSR-011-isomer is a potent anaplastic lymphoma kinase (ALK) inhibitor with an IC50 of 6 nM. This compound demonstrates significant biological activity by undergoing metabolic hydrolysis and NADPH-dependent metabolism, facilitating its clearance in biological systems. TSR-011-isomer is suitable for research focused on ALK-driven cancers, making it a valuable tool for studies in cancer biology and targeted therapy development. -
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. -
ALK Inhibitor
XMU-MP-5 is a selective inhibitor of anaplastic lymphoma kinase (ALK), demonstrating potent inhibitory activity against ALK-mutated Ba/F3 cells with IC50 values ranging from 4 to 50 nM. This compound induces apoptosis specifically in EML4-ALK Ba/F3 cells and has shown notable antitumor efficacy in murine models. XMU-MP-5 serves as a valuable tool in cancer research, particularly in studies focused on ALK-driven malignancies. -
ALK Inhibitor
Ceritinib mesylate is a selective ALK tyrosine kinase inhibitor that functions through ATP-competitive mechanisms, exhibiting an IC50 of 200 pM. In addition to its activity against ALK, Ceritinib mesylate also inhibits IGF-1R, InsR, and STK22D, with IC50 values of 8 nM, 7 nM, and 23 nM, respectively. This compound demonstrates significant antitumor potency, making it a valuable tool for research in cancer biology and targeted therapies. -
BTK Inhibitor
BTK-IN-48 is a potent inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 1.14 μM. This compound effectively inhibits recombinant BTK and c-Src, demonstrating moderate activity against LCK, BMX/ETK, FLT3, and PIM1. BTK-IN-48 is valuable for research related to B-cell malignancies and autoimmune diseases, making it a useful tool for understanding the underlying mechanisms of these conditions. -
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. -
Chemical Probe
MRL-SYKi is a selective chemical probe targeting spleen tyrosine kinase (SYK). It demonstrates potent binding to gain-of-function variants of SYK, with IC50 values of 2.1 nM for SYK(S550Y), 14 nM for SYK(S550F), and 4.6 nM for SYK(P342T) in digitonin-permeabilized cell assays. MRL-SYKi effectively inhibits catalytic activity, achieving IC50 values of 63 nM and 95 nM for SYK(S550F) and SYK(P342T) respectively in phospho-specific assays. This compound is valuable for advancing research on inflammation and related signaling pathways. -
Syk Inhibitor
Sovleplenib is a selective Spleen Tyrosine Kinase (SYK) inhibitor with an IC50 of 25 nM, demonstrating high potency and oral bioavailability. This compound exhibits significant anti-tumor activity and is useful in the research of immune thrombocytopenia (ITP). Its targeted mechanism makes it a valuable tool for studying the roles of SYK in various immune-mediated conditions. -
Syk Inhibitor
Syk-IN-4 is a selective, orally bioavailable inhibitor of SYK, exhibiting an IC50 of 0.31 nM. This compound demonstrates significant potential in modulating immune responses and is being investigated for its therapeutic applications in autoimmunity and hematological malignancies. Syk-IN-4 serves as a valuable tool for researchers exploring the role of SYK in disease progression and treatment strategies. -
Syk Inhibitor
Cevidoplenib is a selective spleen tyrosine kinase (Syk) inhibitor, offering potential anti-inflammatory and immunomodulatory effects. This compound impedes B cell receptor (BCR)-mediated survival, proliferation, and differentiation of B cells, making it useful in research focused on immune responses and related disorders. Additionally, Cevidoplenib demonstrates inhibitory activity on multiple kinases, including Jak2, Jak3, and RET, with varying degrees of potency, providing a versatile tool for investigating kinase signaling pathways in cellular biology. -
Syk Inhibitor
OXSI-2 is a potent Syk inhibitor that exhibits a bioavailable and cell-permeable profile, with an EC50 value of 313 nM and an IC50 of 14 nM. This compound effectively modulates Syk activity, making it a valuable tool for studying signaling pathways in immune responses and cancer. OXSI-2 is suitable for research applications focused on elucidating the role of Syk in disease processes and therapeutic interventions. -
SYK Inhibitor
Lanraplenib succinate is a highly selective, orally active SYK inhibitor with an IC50 of 9.5 nM. It targets SYK activity in platelets through the glycoprotein VI (GPVI) receptor, demonstrating potential therapeutic effects in inflammatory diseases. Notably, Lanraplenib succinate does not prolong bleeding time in preclinical models, indicating a favorable safety profile for clinical applications. -
Syk Inhibitor
Cevidoplenib dimesylate is a selective inhibitor of spleen tyrosine kinase (Syk), demonstrating potential in modulating inflammatory and immune responses. This compound is primarily utilized in research focused on autoimmune diseases and allergic disorders, offering insights into the therapeutic mechanisms of Syk inhibition. Additionally, cevidoplenib may facilitate investigations into the role of Syk in various signaling pathways within the immune system. -
SYK Iinhibitor
ER-27319 maleate is a selective inhibitor of spleen tyrosine kinase (SYK), effectively blocking its tyrosine phosphorylation and subsequent activity. This compound demonstrates significant biological activity by inhibiting the release of antigen-induced allergic mediators from both human and rat mast cells, with an IC50 value of 10 μM. ER-27319 maleate is valuable for research in allergic diseases and inflammation pathways.
