Ephrin Receptor

Tivozanib (KRN951) is an oral VEGFRs 1-3 inhibitor with potential antiangiogenic and cancer-fighting properties.

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

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

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

Tesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor.Cost-effective and quality-assured.

Anti-EphA2 Antibody (MEDI-547 Naked Antibody) is expressed from CHO. The heavy chain type is huIgG1, and the light chain type is hukappa. It has a predicted MW of 145.12 kDa.

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.

UniPR129 is a highly selective, cell-permeable, competitive Eph/ephrin antagonist belonging to the class of L-tryptophan derivatives of lithocholic acid.

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

DS-8895 is a monoclonal antibody targeting EphA2. It enables non-invasive measurement of EphA2 expression within tumors in vivo. DS-8895 can be utilized for studies involving advanced solid cancers that are EphA2 positive.

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.

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

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].

JI-101 hydrochloride is an orally active multi-kinase inhibitor that targets EphB4, VEGFR-2, and PDGFR-β. It exhibits anticancer properties and is applicable in research related to ovarian cancer.

Lithocholic amide-C2-N(didecane) (Compound LC10) is a derivative of lithocholic acid. This compound spontaneously forms lipid nanoparticles in aqueous environments, allowing it to penetrate the skin and reach the dermis, where it exerts anti-inflammatory effects on psoriasis-like chronic skin inflammation. Lithocholic amide-C2-N(didecane) inhibits abnormal keratinocyte proliferation, downregulates the mRNA expression of the psoriasis-related receptor EphA2, and reduces serum levels of various pro-inflammatory factors (such as IL-1α, IL-1β, and IFN-γ) by inhibiting the activation of the Th17/Th2 inflammatory pathways.

Antimalarial agent 37 (compound 33), a selective Type Ⅱ kinase inhibitor, exhibits antiplasmodial activity and demonstrates cytotoxicity towards HepG2 and MCF 7 cancer cells [1].

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.