Catalog No.
Product Name
Application
Product Information
Citations
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EphA2 agonist
123B9 is a potent and selective agonist of the EphA2 receptor, exhibiting a Kd value of 4.0 μM. This compound selectively binds to the ligand-binding domain of the EphA2 tyrosine kinase receptor, facilitating downstream signaling pathways. Importantly, 123B9 does not significantly affect the ligand-binding domains of the closely related EphA3 and EphA4 receptors, making it a valuable tool for targeted studies in cancer research and therapeutic applications involving EphA2 signaling. -
EphA2 Antagonist
UniPR505 is an EphA2 antagonist with an IC50 value of 0.95 µM. This compound exhibits significant anti-angiogenic properties, making it a valuable tool for research related to vascular biology and cancer therapy. Its ability to inhibit the EphA2 receptor pathway allows for potential applications in studying tumor growth and angiogenesis. -
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. -
EphB4 Inhibitor
EphB4-IN-2 is a potent tyrosine kinase inhibitor targeting EphB4, with an IC50 value of 1.6 nM in human assays. This compound demonstrates selective inhibition against kinases containing threonine gatekeeper residues, offering a high degree of ligand efficiency. Its application is valuable in research focusing on EphB4-related signaling pathways and associated therapeutic interventions. -
EphA2 Agonist
EphA2 agonist 2 is a selective agonist targeting the EphA2 receptor, known for its antitumor properties. This compound demonstrates the ability to cross the blood-brain barrier, making it a valuable tool for research in cancer therapeutics and neuro-oncology. Its specificity for EphA2 may aid in elucidating the role of this receptor in tumor progression and could assist in the development of innovative treatment strategies. -
EphB3 Inhibitor
LDN-211904 is a potent and reversible inhibitor of EphB3, with an IC50 of 79 nM, making it a valuable tool for studying EphB3-mediated signaling pathways. It demonstrates good metabolic stability in mouse liver microsomes, indicating its potential for in vivo applications. In research contexts, LDN-211904 may synergize with cetuximab to effectively inhibit STAT3 activation and address colorectal cancer stemness, as well as resistance mechanisms associated with cetuximab treatment. -
EphA4 Receptor Antagonist
EPHA4 antagonist-1 is a selective antagonist of the EphA4 receptor, known for its role in cell signaling, particularly in neuronal development and angiogenesis. This compound effectively inhibits ephrin-A5 binding to the EphA4 Fc receptor with an IC50 value of 10 μM, demonstrating its potency in disrupting EphA4-mediated signaling pathways. The compound's dual action as an EphA2 receptor antagonist expands its utility in biological research, making it valuable for studies on Eph receptor interactions and their implications in cancer and neurobiology. -
EPHB4 Modulator
EPHB4 modulator-1 is a selective modulator of the Ephrin Type-B Receptor 4 (EPHB4), which plays a crucial role in cell signaling and developmental processes. This compound demonstrates significant ability to influence EPHB4-mediated signaling pathways, making it a valuable tool for researching angiogenesis and tumor progression. It is particularly relevant for studies examining the role of EPHB4 in vascular biology and its potential implications in cancer therapy. -
EphA2 Receptor Antagonist
UniPR500 is a competitive antagonist of the EphA2 receptor, exhibiting a Ki value of 0.78 μM. This compound effectively inhibits the binding of biotinylated ephrin-A1 to EphA2 in a dose-dependent manner, with an IC50 of 1.1 μM. UniPR500 is valuable for research applications focusing on cellular signaling pathways and the role of EphA2 in various diseases. -
GFRα-1 Agonist
(E)-Aminoquinol is a selective agonist of the GFRα-1 receptor. It mimics the neurotrophic effects of glial cell-derived neurotrophic factor (GDNF) and promotes Ret autophosphorylation in Neuro-2A cells. This compound is particularly relevant for research focused on neurodegenerative disorders such as Parkinson’s disease, facilitating studies on neuronal survival and growth pathways. -
GFRα-1 Agonist
Aminoquinol is a GFRα-1 agonist that mimics the neurotrophic effects of glial cell line-derived neurotrophic factor (GDNF). It induces Ret autophosphorylation in Neuro-2A cells, promoting neuronal survival and differentiation. This compound is applicable in research concerning neurodegenerative disorders, particularly Parkinson's disease. -
GFRα-1 Agonist
Aminoquinol phosphate is a GFRα-1 agonist that mimics the neurotrophic effects of glial cell-derived neurotrophic factor (GDNF). This compound induces Ret autophosphorylation in Neuro-2A cells, highlighting its potential role in neuroprotection. Aminoquinol phosphate is suitable for research applications related to Parkinson's disease and other neurodegenerative disorders, offering insights into mechanisms of neuronal survival and growth. -
GFRα-1 Agonist
Aminoquinol triphosphate is a potent GFRα-1 agonist that induces neurotrophic effects akin to Glial Cell-Derived Neurotrophic Factor (GDNF). This compound promotes Ret autophosphorylation in Neuro-2A cells, making it a valuable tool in research focused on neurodegenerative disorders, particularly Parkinson's disease. Its mechanism of action positions it as a promising candidate for studies exploring neuroprotection and neuronal survival. -
ITK Inhibitor
Soquelitinib is a selective covalent inhibitor of interleukin-2-inducible kinase (ITK). It exhibits significant anti-inflammatory activity across multiple models of T cell-mediated inflammatory diseases, including asthma, pulmonary fibrosis, systemic sclerosis, psoriasis, and acute graft-versus-host disease. By inhibiting Th2 cytokine production, Soquelitinib enhances the infiltration of CD8+ T cells into tumors, promoting improved T effector function and potential therapeutic benefits in oncology and immunology research. -
ITK Inhibitor
GNE-9822 is a potent and selective inhibitor of ITK (Interleukin-2-inducible T-cell kinase) with a Ki value of 0.7 nM and an EC50 value of 354.5 nM. This compound demonstrates favorable ADME properties, making it suitable for in vivo studies. GNE-9822 is primarily utilized in research on asthma and other related immunological conditions, providing insights into the modulation of T-cell signaling pathways. -
ITK Inhibitor
ITK inhibitor 6 is a highly selective inhibitor of ITK with an IC50 of 4 nM. This compound also demonstrates weaker activity against BTK, JAK3, EGFR, and LCK, with IC50 values of 133 nM, 320 nM, 2360 nM, and 155 nM, respectively. ITK inhibitor 6 effectively inhibits the phosphorylation of PLCγ1 and ERK1/2 pathways and exhibits significant antiproliferative activity. It is a valuable tool for research applications focused on lymphocyte signaling and cancer biology. -
ITK Inhibitor
ITK-IN-6 is a potent and selective inhibitor of Interleukin-2-inducible T-cell kinase (ITK), with a Kd of 387 nM. It directly targets the ITK kinase domain, effectively blocking the release of pro-inflammatory cytokines and modulating the activation and differentiation of Th2 and Th17 cells. This compound demonstrates significant potential in asthma research by reducing inflammatory cell infiltration, mucus production, and IgE levels, thereby mitigating airway inflammation and improving asthma progression. -
ITK Inhibitor
ITK inhibitor 5 is a selective inhibitor targeting the interleukin-2-inducible T-cell kinase (ITK) with an IC50 of 5.6 nM. Demonstrating low activity against Bruton's tyrosine kinase (BTK) with an IC50 of 25 nM, this compound is useful in studying T-cell signaling pathways and immune responses. It serves as an effective tool in research aimed at understanding the role of ITK in various hematological disorders and inflammatory diseases. -
Itk Inhibitor
ITK/TRKA-IN-1 is a selective inhibitor targeting IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA), exhibiting an IC50 of 1.0 nM for ITK and achieving 96% inhibition of TRKA. This compound is valuable for investigating the roles of ITK and TRKA in immune responses and neurobiology. Its dual inhibitory action positions it as a significant tool for research in cancer immunotherapy and neurodegenerative disease studies, enabling the exploration of signaling pathways associated with these kinases. -
ITK Antagonist
ITK antagonist is a selective inhibitor of Interleukin-2 inducible T-cell kinase (ITK) with an IC50 value of 1 nM and 20 nM in various assays. This compound is orally active and has shown the ability to inhibit insulin receptor kinase (IRK) with an IC50 of 160 nM. It is valuable for research applications focused on T-cell signaling pathways and the modulation of immune responses. -
AXL Inhibitor
Axl-IN-20 is a selective AXL inhibitor with a potent IC50 of 5 nM. This orally active compound demonstrates significant anti-tumor activity, particularly against hematological malignancies. It is a valuable tool for research applications aimed at understanding AXL signaling pathways and developing targeted cancer therapies. -
TAM Receptor Inhibitor
TAM-IN-1 is a potent macrocyclic inhibitor targeting TAM receptors Axl and Mer, displaying binding affinities with Kis of 130 pM and <50 pM, respectively. This compound demonstrates significant biological activity in modulating pathways associated with tumor progression and immune evasion. TAM-IN-1 is applicable in research focused on cancer therapeutics and the study of receptor-mediated signaling in the tumor microenvironment. -
TYRO3 Inhibitor
UNC9426 is a highly selective inhibitor of TYRO3, exhibiting an IC50 of 2.1 nM and demonstrating 276-fold and 90-fold selectivity over MERTK and AXL, respectively. This compound effectively reduces platelet aggregation without prolonging bleeding time, and it inhibits TYRO3-mediated processes in both tumor cells and macrophages. With a favorable safety profile, UNC9426 is an invaluable tool for investigating TYRO3-dependent phenotypes, including applications in non-small cell lung cancer (NSCLC) research. -
AXL Inhibitor
Ligritinib is an AXL receptor tyrosine kinase inhibitor that displays oral bioavailability. It effectively inhibits AXL kinase activity, disrupting downstream signaling pathways associated with cancer progression. Ligritinib is particularly relevant in cancer research, and it is often investigated in combination with chemotherapy for the treatment of non-small cell lung cancer (NSCLC). -
MER/AXL Inhibitor
BPR5K230 is a dual inhibitor targeting the receptor tyrosine kinases MER and AXL, exhibiting IC50 values of 4.1 nM and 9.2 nM, respectively. This compound effectively inhibits the proliferation of Ba/F3-MER cells, with an IC50 of 5 nM. In preclinical models, BPR5K230 demonstrates anti-inflammatory and antitumor activities against various cancer cell lines, including 4T1, MDA-MB-231, MC38, and Hepa1-6, as well as favorable pharmacokinetic properties in mice. These attributes make BPR5K230 a valuable tool for research into cancer biology and targeted therapies. -
TAM Receptor Inhibitor
AZ14145845 is a selective inhibitor targeting the TAM receptor kinases Mer and Axl, classified as a type I1/2 dual kinase inhibitor. This compound demonstrates notable in vivo efficacy, making it a valuable tool for research in cancer biology and therapeutic resistance mechanisms. Its selective inhibition of the TAM receptors contributes to the modulation of immune responses and potential enhancement of antitumor activity, serving as a significant asset in studies focused on cancer treatment and immunotherapy. -
Axl Inhibitor
TL4830031 is a potent Axl inhibitor, exhibiting an IC50 value of 26 nM. This compound effectively disrupts Axl phosphorylation, leading to inhibition of cell invasion and migration. TL4830031 is an ideal reagent for cancer research applications, providing valuable insights into tumor biology and potential therapeutic interventions targeting the Axl pathway. -
AXL Inhibitor
Axl-IN-6 is a potent AXL inhibitor that demonstrates significant anti-tumor activity. This orally active compound effectively inhibits tumor growth in the MV-4-11 subcutaneous xenograft model, showcasing its potential for cancer research applications. Axl-IN-6 is well tolerated, making it a suitable candidate for evaluating AXL targeting in therapeutic studies. -
MerTK Inhibitor
MerTK-IN-3 is a selective MerTK inhibitor, demonstrating an IC50 of 21.5 nM for MerTK while maintaining a significantly higher IC50 of 991.3 nM for Tyro3. This compound is suitable for research applications focused on colon cancer, enabling studies into MerTK's role in tumor progression and potential therapeutic interventions. Its oral bioavailability further enhances its utility in preclinical studies. -
AXL Inhibitor
Axl-IN-9 is a potent inhibitor of AXL, exhibiting an IC50 of 26 nM. This compound demonstrates excellent transmembrane and pharmacokinetic properties, making it suitable for in vivo studies. Axl-IN-9 is intended for research applications in proliferative diseases, autoimmune disorders, allergic reactions, inflammatory conditions, transplant rejection, cancer, and other related mammalian diseases. -
AXL Inhibitor
Axl-IN-11 is a potent AXL inhibitor that targets the AXL receptor tyrosine kinase. It exhibits significant biological activity in the modulation of cell proliferation and migration, making it useful in the study of various proliferative and autoimmune diseases, as well as in cancer research. Additionally, Axl-IN-11 can be applied in the investigation of allergic, inflammatory, and viral infectious diseases, as well as transplant rejection mechanisms in mammals. -
AXL Inhibitor
Axl-IN-4 is an AXL kinase inhibitor that demonstrates an IC50 of 28.8 μM. This compound specifically targets the AXL receptor tyrosine kinase, which is implicated in multiple cancer pathways and immune responses. Axl-IN-4 is useful for research applications aiming to elucidate the roles of AXL in tumor progression and to explore potential therapeutic strategies against AXL-driven malignancies. -
AXL inhibitor
Axl-IN-17 is a selective AXL inhibitor that demonstrates potent inhibitory activity with an IC50 value of 3.2 nM. This compound exhibits significant antitumor efficacy, making it a valuable tool for research in cancer biology. Axl-IN-17 is suitable for studies focusing on AXL-mediated signaling pathways and their implications in tumor progression and metastasis. -
AXL Inhibitor
Axl-IN-10 is a potent AXL inhibitor with an IC50 of 5 nM, effectively targeting the AXL receptor. This compound exhibits favorable transmembrane and pharmacokinetic properties, enhancing its utility in biological research. Axl-IN-10 is applicable in the study of various proliferative diseases, autoimmune disorders, allergic reactions, inflammatory conditions, transplant rejection, and cancer, making it a valuable tool for researchers exploring these complex pathologies in mammals. -
MerTK Inhibitor
UNC3133 is a selective and orally bioavailable inhibitor of the Mer tyrosine kinase (MerTK), demonstrating an IC50 of 8.1 nM. This compound exhibits preferential inhibition of the TAM receptor family, particularly with approximately sevenfold selectivity for Axl and tenfold selectivity for Tyro3, while also showing comparable activity against Flt3. UNC3133 is applicable in research focused on anti-tumor and anti-infection mechanisms, providing insights into therapeutic strategies targeting these pathways. -
AXL Inhibitor
Axl-IN-12 is a potent AXL inhibitor that selectively targets the AXL receptor tyrosine kinase. It exhibits significant biological activity in regulating cell proliferation and modulating immune responses. Axl-IN-12 is suitable for research applications related to proliferative diseases, autoimmune disorders, allergic responses, inflammation, transplant rejection, various malignancies, and viral infections in mammalian systems. -
Axl Inhibitor
AXL-IN-15 is a highly potent inhibitor of the Axl receptor tyrosine kinase, exhibiting Ki and IC50 values of less than 1 nM. This compound is valuable for research focused on cancer biology, particularly in studies investigating Axl's role in tumor progression and metastasis. AXL-IN-15 can aid in elucidating the molecular mechanisms underlying Axl-mediated signaling pathways and their implications in various malignancies. -
AXL Inhibitor
Axl-IN-7 is a potent inhibitor of the AXL receptor tyrosine kinase. This compound demonstrates significant activity in targeting AXL-mediated signaling pathways, making it valuable for investigating AXL-related diseases, including various cancers such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors. Additionally, Axl-IN-7 has potential applications in research focused on renal diseases, immune system disorders, and cardiovascular conditions. -
MerTK/Axl Inhibitor
MerTK/Axl-IN-1 is a highly selective dual inhibitor targeting MerTK and Axl receptors, demonstrating potent inhibitory activity with IC50 values of 4.2 nM and 8.8 nM in Ba/F3 cells, and 0.2 nM and 0.9 nM in HTRF assays. This compound effectively inhibits phosphorylated MerTK (pMerTK) in vivo, indicating its utility in biological research. With a prolonged half-life and favorable oral bioavailability, MerTK/Axl-IN-1 is suitable for studies in cancer biology and therapeutic development aimed at disruptions in MerTK and Axl signaling pathways. -
AXL Inhibitor
Axl-IN-19 is a selective inhibitor of AXL, a membrane-bound receptor tyrosine kinase, exhibiting an IC50 of 5.3 nM and a cellular KD of 6.8 nM. This compound demonstrates favorable pharmacokinetic properties in rats, characterized by low clearance and moderate bioavailability. Axl-IN-19 is primarily utilized in cancer research to explore the role of AXL signaling in tumor progression and metastasis. -
TAM Receptor Inhibitor
MerTK-IN-1 is an inhibitor of the MerTK receptor, a critical target in the regulation of tumor-associated macrophages (TAMs). This compound demonstrates the ability to effectively bind to MerTK in vivo, providing valuable insight into immune modulation in tumor microenvironments. MerTK-IN-1 is suitable for research applications focused on cancer immunotherapy and the role of macrophages in tumor progression. -
Gas6/Axl Inhibitor
Anticancer agent 109 is a Gas6/Axl inhibitor that demonstrates significant anti-cancer activity. This compound effectively downregulates the expression of Gas6 and Axl, which in turn reduces the activation of p-PI3K and p-AKT in cancer cells. Anticancer agent 109 induces G1 phase cell cycle arrest and promotes apoptosis, leading to substantial inhibition of tumor growth in nude mouse models. This reagent is suitable for research focused on cancer biology and therapeutic development targeting the Gas6/Axl signaling pathway. -
TYRO3/MERTK Inhibitor
UNC9435 is a dual inhibitor of TYRO3 and MERTK, exhibiting IC50 values of 3.7 nM and 1.1 nM, respectively. This compound has been shown to significantly reduce colony formation in non-small cell lung cancer cultures, indicating its potential as a therapeutic agent in cancer research. UNC9435 may also serve as a useful tool for studying the role of TYRO3 and MERTK in various biological processes and disease mechanisms. -
AXL Inhibitor
Axl-IN-3 is a selective inhibitor of the AXL kinase, demonstrating potent activity with an IC50 of 41.5 nM. This compound has shown minimal inhibition of other kinases, making it an ideal choice for studies focused on AXL-mediated signaling pathways. Axl-IN-3 is suitable for research applications involving cancer biology, immune modulation, and therapeutic resistance studies. -
MERTK/AXL Inhibitor
UNC8969 is a dual inhibitor targeting MERTK and AXL, exhibiting IC50 values of 1.1 ± 0.8 nM for MERTK and 5.3 ± 2.7 nM for AXL. With a half-life (T1/2) of 7.3 hours following intravenous administration at 5 mg/kg in mice, UNC8969 demonstrates significant biological activity. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating the roles of MERTK and AXL in tumor progression and immune modulation. -
AXL Inhibitor
AXL-IN-14 is a highly potent, orally bioavailable inhibitor of AXL, exhibiting an impressive IC50 value of 0.8 nM. This compound effectively disrupts Gas6/AXL-mediated cell migration and invasion while reducing the expression levels of phospho-AXL and phospho-AKT proteins. AXL-IN-14 demonstrates significant anti-tumor activity, making it a valuable tool for research in cancer therapeutics and metastasis studies. -
AXL Inhibitor
Axl-IN-5 is a selective inhibitor of AXL, exhibiting an IC50 of 283 nM. This compound demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology. Axl-IN-5 can be utilized to study the role of AXL signaling in tumor progression and to investigate potential therapeutic strategies targeting the AXL pathway in various malignancies. -
MET/AXL Inhibitor
(Z)-S49076 hydrochloride is a potent inhibitor of MET and AXL, effectively disrupting their downstream signaling pathways. This compound demonstrates significant biological activity by inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. Additionally, (Z)-S49076 hydrochloride addresses resistance mechanisms associated with epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in Erlotinib-resistant cell lines. It is a valuable tool for research in non-small cell lung cancer (NSCLC). -
AXL Inhibitor
Denfivontinib hydrochloride is an AXL inhibitor that exerts synergistic antitumor effects when used in combination with the PD-1 inhibitor Pembrolizumab. This compound enhances the NOD-like receptor pathway, facilitating the formation of the NLRP3 inflammasome. Its unique mechanism of action makes it a valuable tool for cancer research, particularly in studying immune modulation and tumor progression. -
AXL Inhibitor
ER-851 is a selective inhibitor of AXL with an IC50 of 100 nM, demonstrating potent oral bioactivity. It has been shown to exhibit antitumor effects, making it a valuable compound for research in cancer biology and therapeutic development. Its selectivity and efficacy position ER-851 as a critical tool for studying AXL's role in tumor progression and metastasis.
