epha-2

UniPR505 is a potent EphA2 antagonist (IC50: 0.95 µM), a novel 3α-carbamoyloxy derivative with antiangiogenic properties.

Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.

Agerafenib hydrochloride, a highly potent inhibitor of BRAFV600E (Kd: 14 nM), demonstrates significant efficacy.

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

EphA2 agonist 2 (Lead compound) is a selective agonist targeting the EphA2 receptor, with antitumor properties and the ability to cross the blood-brain barrier (BBB).

EphA2 Agonist 1 (Compound 7bg) is a potent and selective EphA2 receptor agonist, demonstrating significant efficacy in targeting overexpressed EphA2 glioblastoma cells and inducing EphA2 phosphorylation [1].

EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2, EPHA4, and GAK, exhibiting KD values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. The predicted half-life of EPHA2/A4/GAK-IN-1 in microsomal stability tests measures 4.6 hours. Additionally, this compound has antiviral efficacy, capable of preventing Dengue virus infection in Huh7 hepatocytes.

Anti-EphA2 Antibody is a human-derived antibody expressed in CHO cells, specifically targeting EphA2. Its predicted molecular weight (MW) is 150 kDa. For isotype control, refer to Human IgG1 kappa, Isotype Control.

Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.

UniPR129 is a competitive Eph-ephrin antagonist agent that acts by blocking in vitro angiogenesis at low micromolar concentrations.

NG25 is a potent dual inhibitor of TAK1 and MAP4K2, with IC50s of 149 nM and 21.7 nM, respectively.