Ephrin Receptor

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.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

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 c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.

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

UniPR1447 is a dual antagonist for both EphA2 and EphB2 receptors, exhibiting an IC50 value of 6.6 μM against EphA2-ephrin-A1 binding [1].

123C4 is a potent, selective, and competitive agonist of the receptor tyrosine kinase EPHA4 (Ki=0.65 μM)[1].

ALW-II-41-27 (Eph receptor tyrosine kinase inhibitor), an Eph receptor tyrosine kinase inhibitor, is used for cancer therapy.

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

UniPR500, a derivative of UniPR129, is a competitive antagonist for the EphA2 receptor, with a Ki of 0.78 μM. It reduces the binding of biotinylated Ephrin-A1 to EphA2 in a dose-dependent manner, exhibiting an IC50 value of 1.1 μM.

PKMYT1-IN-8 (Compound 137) is an inhibitor of PKMYT1, with an IC50 value of 9 nM. It also inhibits EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2, exhibiting IC50 values of 1.79, 3.17, 4.29, 6.32, 6.83, 8.10, and 10.9 μM, respectively. Additionally, PKMYT1-IN-8 suppresses the proliferation of cancer cells OVCAR3 with a GI50 of 2.02 μM.

Ifabotuzumab (KB-004) is an antibody targeting EphA3+ cells, significantly reducing CCR10+ cells and improving pulmonary fibrosis in humanized NSG mice.

AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM. AZ12672857 inhibits cell proliferation of Src transfected 3T3 cells with IC50 of 2 nM and autophosphorylation of EphB4 in transfected CHO-K1 cells with IC50 of 9 nM.

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.

Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.

JI-101 (CGI-1842) is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 (EphB4).

AWL-II-38.3 is a highly potent EphA3 inhibitor with potent kinase inhibitory activity against EphA3 but no significant cellular activity against Src family kinases or b-raf.

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

KYL acetate is an EphA4 receptor tyrosine kinase inhibitor (Kd = 0.8 μM); inhibits EphA4-EphrinA5 interactions (IC50 = 6.34 μM). Prevents AβO induced synaptic damage, dendritic spine loss and prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. Exhibits a long half life in cell culture media (8 and 12 hours in PC3 and C2C12 media respectively). Neuroprotective.

Tesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor with IC50 values ​​of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4.

LDN-211904 oxalate (LDN211904 oxalate) is a selective and efficient EphB3 inhibitor with antitumor activity, useful in neurodegenerative disease research.

Urolithin D is a competitive and selective reversible antagonist of the EphA receptor, an ellagitannin colonic metabolite that inhibits EphA2 phosphorylation in prostate cancer cells, attenuates triglyceride accumulation in adipocytes and hepatocyte cultures, and may be used in the study of metabolic disorders.

N-Lithocholyl-L-alanine, a bile acid conjugate, also serves as an inhibitor of the ephrin type-A receptor 2 (EPHA2) with an IC50 value of 19.95 µM.