Ephrin Receptor

ALW-II-49-7 is a selective and potent inhibitor of EphB2 kinase with an EC50 value of 40 nM in cell.

Targefrin: potent EphA2 antagonist, binds with 21nM Kd, IC50 of 10.8nM, induces receptor degradation in pancreatic cancer cells.

(123B9)2-Motif is a selective agonist of the EphA2 receptor with a dissociation constant (Kd) of 4.9 μM and does not bind to EphA4. It functions by inducing phosphorylation and oligomerization of the EphA2 receptor, promoting receptor activation and internalization. (123B9)2-Motif is primarily used in research on targeted drug delivery for cancers overexpressing EphA2, such as breast cancer, to reduce circulating tumor cells and inhibit metastasis.

(123B9)2-L2-PTX is an EphA2 agonist peptide-drug conjugate (PDC). It consists of dimer 123B9 and Paclitaxel. This compound significantly reduces circulating tumor cells and inhibits lung metastasis in a breast cancer metastasis mouse model. (123B9)2-L2-PTX is applicable in cancer research, including studies on melanoma, ovarian cancer, and breast cancer.

SA-PA, a self-assembled intracellular PROTAC leveraging azide-alkyne click chemistry, selectively degrades VEGFR-2, PDGFR-β, and EphB4 proteins within U87 cells

AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM.

AWL-II-38.3 is a highly potent EphA3 inhibitor with potent kinase inhibitory activity against EphA3.Cost-effective and quality-assured.

A11 (ANXA1-derived 11 amino acid-long peptide) acetate is an ANXA1-EphA2 interaction inhibitor peptide. It reduces the binding of ANXA1 to EphA2 and enhances the binding of Cbl (E3 ubiquitin ligase of EphA2) to EphA2. A11 acetate effectively lowers EphA2 levels, significantly increases its ubiquitination, facilitates EphA2 internalization, and promotes colocalization of EphA2 and Cbl in nasopharyngeal carcinoma (NPC) cells. Additionally, A11 acetate inhibits NPC cell proliferation, migration, invasion, and angiogenesis.

UniPR1449 is an EphA2 receptor antagonist with a KD of 3.8±2.4 μM, which is significant in cancer pathophysiology [1].

EphA4 inhibitor, Kd 0.8 μM, blocks EphA4-EphrinA5; avoids AβO damage, preserves spines & LTP; long half-life (8-12h), neuroprotective.

UniPR1454 targets the EphA2 receptor and inhibits the interaction between EphA2 and ephrin A1, with an IC50 of 2.6 μM. Furthermore, UniPR1454 suppresses the proliferation of glioblastoma U251 cells.

Compound 7bg is a potent, selective EphA2 agonist targeting overexpressed glioblastoma cells.

123B9 is a tumor-homing agent characterized as a potent and selective agonist for EphA2 with a dissociation constant (Kd) of 4.0 μM. It specifically targets the ligand-binding domain of the EphA2 tyrosine kinase receptor. Notably, 123B9 does not significantly inhibit the ligand-binding domains of closely related receptors EphA3 and EphA4.

APY-d3 is an EphA4-LBD antagonist peptide with a Kd value of 138 nM. It is constrained in a biologically active β-hairpin conformation through a disulfide bond linking its ends. APY-d3 is applicable for research in cancers such as gastric and pancreatic cancer, as well as in neurodegenerative diseases like amyotrophic lateral sclerosis and Alzheimer's disease.

Anti-EphB2 Antibody serves as a functional therapeutic tool specifically designed to enable the precise detection and neutralization of the EphB2 protein which plays a pivotal role in the orchestration of cell positioning and cancer progression during strictly monitored laboratory observation periods and molecular investigations to evaluate the pharmacological potential of targeted RTK inhibition.

Eph inhibitor 2 is an Eph family tyrosine kinase inhibitor targeting Eph receptors.

NVP-BHG712 isomer shows conserved non-bonded binding to EPHA2 and EPHB4.

JI-101 (CGI-1842) is an oral multi-kinase inhibitor that targets VEGFR-2, PDGFR-β, and EphB4.

NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and

EphA4 inhibitor, Kd: 0.8 μM, IC50: 6.34 μM. Protects synapses and spines, maintains LTP. Long half-life: 8-12h. Neuroprotective.