Ephrin Receptor

ALW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor.

NVP-BHG712 isomer, a regioisomer of NVP-BHG712, shows conserved non-bonded binding to EPHA2 and EPHB4.

UniPR1331 is an orally active 3β-hydroxy-Δ5-choline acid derivative that targets Eph-ephrin interactions. By inhibiting the interaction between VEGFR2 and its ligand, vascular endothelial growth factor, UniPR1331 effectively dampens autophosphorylation, subsequent signaling, and pro-angiogenic activation in endothelial cells. This compound demonstrates significant anti-angiogenic, anti-cancer, and anti-inflammatory properties, making it suitable for research applications in cancer and inflammation, including glioma and colitis.

ALW-II-49-7 is a selective inhibitor of the EphB2 kinase, exhibiting an EC50 value of 40 nM in cellular assays. It is designed to effectively disrupt EphB2 signaling pathways, which are implicated in various biological processes including cell adhesion and migration. This reagent is valuable for research applications focusing on cancer biology, neurodevelopment, and the modulation of angiogenesis.

AWL-II-38.3 is a selective inhibitor of the ephrin-A receptor (EphA3) kinase. This compound demonstrates potent inhibitory activity specifically targeting EphA3 while displaying minimal effects on Src-family kinases and b-raf. Its specificity makes AWL-II-38.3 valuable for research applications involving EphA3-mediated signaling pathways and related cellular processes.

LDN-211904 oxalate is a potent and reversible inhibitor of EphB3, exhibiting an IC50 of 79 nM. This compound demonstrates favorable metabolic stability in mouse liver microsomes, making it suitable for in vitro studies. LDN-211904 oxalate is particularly relevant for research involving STAT3-activated colorectal cancer stemness and may help overcome Cetuximab resistance in colorectal cancer.

150D4 is a selective agonist of EphA4, capable of effectively penetrating the blood-brain barrier. This compound exhibits excitatory activity and provides neuroprotective effects, making it a valuable tool for studying various neurological conditions. Its unique properties make 150D4 suitable for research aimed at understanding the role of EphA4 in neurobiology and developing potential therapeutic strategies.

EphA2 Agonist 1 is a selective agonist for the EphA2 receptor, demonstrating high potency in stimulating EphA2 phosphorylation. This compound exhibits significant effectiveness against glioblastoma cells that overexpress the EphA2 receptor, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to activate EphA2 pathways can aid in elucidating the receptor's role in tumorigenesis and potential interventions.

UniPR129 is a potent, orally active antagonist of Eph/ephrin interactions. It effectively inhibits the EphA2-ephrin-A1 interaction with an IC50 of 945 nM and a Ki of 370 nM. This compound has demonstrated the ability to inhibit angiogenesis and exhibits both antitumor and neuroprotective properties. UniPR129 is suitable for research applications in cancer and neurological disorders, including colorectal cancer and optic neuropathy.

Eph Inhibitor 1 is a potent inhibitor of Eph receptors, targeting the Eph family of receptor tyrosine kinases. It has demonstrated significant biological activity in modulating cellular signaling pathways involved in neural development and synaptic plasticity. This compound holds promise for research applications related to neurological disorders, facilitating insights into therapeutic strategies for conditions linked to Eph receptor dysregulation.

EphA2 antagonist 1 is an ephrin type-A receptor 2 (EPHA2) inhibitor designed to modulate the signaling pathways associated with this receptor. It exhibits significant biological activity in disrupting EPHA2-mediated processes, which may have implications in cancer research and metastasis studies. This compound serves as a valuable tool for investigating the role of EPHA2 in various cellular contexts and therapeutic applications.

Targefrin is a potent EphA2-targeting agent that functions as an antagonist. It exhibits high affinity for the EphA2 ligand-binding domain, with a dissociation constant of 21 nM and an IC50 value of 10.8 nM. Targefrin induces internalization and degradation of the EphA2 receptor in various pancreatic cancer cell lines, making it a valuable tool for research on cancer biology and therapeutic targeting of EphA2-related pathways.

UniPR1447 is a dual antagonist of EphA2 and EphB2, exhibiting an IC50 of 6.6 μM for the inhibition of the EphA2-ephrin-A1 interaction. This compound serves as a valuable tool in research focused on the role of Eph receptors in cellular processes such as angiogenesis, tumor progression, and neural development. Its application in studies targeting EphA2 and EphB2 signaling pathways contributes to understanding their implications in various diseases, making UniPR1447 a relevant reagent for therapeutic exploration.

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.

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-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 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.

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 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-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.

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.