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Catalog No.
Product Name
Application
Product Information
Citations
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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-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. -
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. -
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. -
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 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. -
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. -
SYK Iinhibitor
ER-27319 is a potent and selective Spleen Tyrosine Kinase (SYK) inhibitor, known for its ability to suppress the tyrosine phosphorylation of SYK and thereby inhibit its enzymatic activity. This compound effectively blocks the release of antigen-induced allergic mediators from human and rat mast cells, exhibiting an IC50 of 10 μM. ER-27319 is a valuable tool for research in the field of allergic diseases, particularly in studies focused on mast cell activation and modulation. -
Syk Inhibitor
Syk-IN-1 is a highly potent inhibitor of Syk (spleen tyrosine kinase), demonstrating an IC50 value of 35 nM. This compound effectively disrupts Syk-mediated signaling pathways, making it valuable for studies involving immune response, cell proliferation, and apoptosis. Syk-IN-1 is suitable for research applications focused on hematological malignancies and inflammatory diseases, facilitating the exploration of Syk's role in various biological processes. -
SYK/ZAP70 Inhibitor
(R,S)-MK-8457 is a dual inhibitor of SYK and ZAP70, key signaling molecules involved in immune cell activation. This compound exhibits potent inhibitory activity, making it a valuable tool for investigating the pathophysiology of autoimmune disorders. Its application in research focuses primarily on the study of rheumatoid arthritis and other inflammatory conditions. -
SYK Inhibitor
Lanraplenib monosuccinate is a highly selective inhibitor of spleen tyrosine kinase (SYK), with an IC50 of 9.5 nM. This compound inhibits SYK activity in platelets through the glycoprotein VI (GPVI) receptor, making it a promising candidate for the treatment of inflammatory diseases. Notably, lanraplenib monosuccinate does not prolong bleeding time in preclinical models, indicating a favorable safety profile for potential therapeutic applications. -
Syk Inhibitor
Syk-IN-8 is a selective Syk inhibitor that exhibits significant antiproliferative activity against various hematological tumor cell lines. By targeting and inhibiting the phosphorylation of PLCγ2, Syk-IN-8 serves as a valuable tool for investigating the molecular mechanisms underlying blood cancers and evaluating potential therapeutic strategies. Its specificity and efficacy make it an important reagent for researchers focused on hematological malignancies. -
SYK Inhibitor
BI 894416 is a selective inhibitor of spleen tyrosine kinase (SYK), a key regulator involved in various immune responses. This compound is particularly relevant for studying the pathophysiology of severe asthma, making it valuable in the development of therapeutic strategies. Additionally, BI 894416 features a deuterium-labeled derivative, which serves as an internal standard in bioanalytical applications, enhancing the accuracy of quantitative assessments in research settings. -
Syk Inhibitor
Syk-IN-7 is a selective inhibitor of spleen tyrosine kinase (SYK). It demonstrates significant inhibition of SYK activity, thereby impacting B-cell receptor signaling pathways and immune responses. This compound is valuable for studying the roles of SYK in immunological research and potential therapeutic applications in autoimmune diseases and lymphoid malignancies. -
Syk Inhibitor
Syk-IN-2 is a selective inhibitor of spleen tyrosine kinase (Syk), a vital signaling molecule in various hematopoietic cells. Its inhibition modulates immune responses and has been implicated in the treatment of autoimmune diseases and certain cancers. This compound serves as a valuable tool for researchers investigating Syk-related pathways and potential therapeutic interventions. -
SYK Inhibitor
NMS-0963 is a potent inhibitor of spleen tyrosine kinase (SYK), exhibiting an oral bioavailability and an IC50 value of 3 nM. This compound effectively inhibits the proliferation of BaF3-TEL/SYK cell lines at a concentration of 27 nM, making it a valuable tool for investigating SYK-related pathways in various biological contexts and potential therapeutic applications in diseases involving SYK dysregulation. -
Spleen Tyrosine Kinase Inhibitor
BI1002494 is a selective inhibitor of spleen tyrosine kinase (SYK) with oral bioavailability. It demonstrates potent inhibitory activity with an IC50 of 115 nM against high-affinity IgE receptor-mediated degranulation in mast cells and basophils. This compound is a valuable tool for studying immune responses and can be applied in a variety of immunology research applications. -
Syk Inhibitor
Type-II-IN-1 is a potent type II inhibitor of spleen tyrosine kinase (Syk), exhibiting an IC50 value of 2.1 nM. It specifically interacts with the DFG-out conformation of Syk, making it a valuable tool for the study of immunological processes. This compound is particularly relevant for research applications related to asthma and other immune-related disorders. -
Syk Inhibitor
Syk-IN-13 is a selective inhibitor of Spleen tyrosine kinase (Syk). It has demonstrated significant biological activity in modulating immune responses and inflammatory pathways, making it a valuable tool for researching conditions such as rheumatoid arthritis and systemic lupus erythematosus. This compound allows for the exploration of Syk's role in various cellular processes, highlighting its potential as a therapeutic target in autoimmune diseases. -
Syk Inhibitor
Syk-IN-11 is a selective inhibitor of Spleen tyrosine kinase (Syk) with a reported IC50 of 13 nM. This compound demonstrates significant biological activity and has applications in the research of autoimmune disorders such as arthritis, as well as hematological malignancies like chronic lymphocytic leukemia. Its role in modulating Syk signaling pathways makes it a valuable tool for elucidating disease mechanisms and developing potential therapeutic strategies. -
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. -
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.
