EphA Inhibitor

UniPR1331 is an orally active 3β-hydroxy-Δ5-choline acid derivative that inhibits Eph-ephrin interactions. UniPR1331 blocks the interaction of VEGFR2 with its natural ligand vascular endothelial growth factor and inhibits subsequent autophosphorylation, signaling, and pro-angiogenic activation of endothelial cells. UniPR1331 exhibits anti-angiogenesis, anti-cancer and anti-inflammation effects. UniPR1331 can be used for the researches of cancer and inflammation, such as glioma and colitis.

APY-d3 is a highly selective EphA4 receptor inhibitor, with an IC₅₀ value of 17-56 nM for human EphA4, an IC₅₀ value of 20 nM for mouse EphA4, and a K_d value of 138 nM for EphA4-LBD. APY-d3 binds to EphA4, blocks its interaction with ephrin ligands, inhibits tyrosine phosphorylation of EphA4, prevents growth cone collapse, and does not induce EphA4 phosphorylation in primary cortical neurons. APY-d3 adopts a β-hairpin conformation stabilized by an N-terminal to C-terminal disulfide bond. APY-d3 can be used in research related to amyotrophic lateral sclerosis, Alzheimer's disease, stroke, neurodegenerative diseases and cancer.

DS-8895(DS-8895A) is an anti-EphA2 monoclonal antibody with specific binding to EphA2 receptors and EphA2-expressing cells. DS-8895, when conjugated with ⁸⁹Zr, ¹¹¹In, or ¹²⁵I, supports molecular imaging of EphA2 expression in xenograft models. DS-8895 allows noninvasive measurement of EphA2 expresssion in tumors in vivo..

MBRC-101 Antibody is a human monoclonal antibody targeting EphA5. MBRC-101 Antibody can be used to synthesize the ADC MBRC-101.

Lithocholic amide-C2-N(didecane) (Compound LC10) is a Lithocholic acid (HY-B0172) analogue. Lithocholic amide-C2-N(didecane) can form lipid nanoparticles spontaneously in the aqueous milieu, permeate through the skin, penetrate the deeper dermal layers, and exert anti-inflammatory effects against psoriasis-like chronic skin inflammations. Lithocholic amide-C2-N(didecane) can inhibit abnormal proliferation of keratinocytes, downregulate the mRNA expression of the psoriasis-associated receptor EphA2 and reduce serum levels of multiple pro-inflammatory factors such as IL-1α, IL-1β, and IFN-γ by inhibiting activation of the Th17/Th2 inflammatory pathway.