2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Ephrin Receptor
  5. EphA Isoform

EphA

EphA receptors are receptor tyrosine kinases that bind cell-surface ephrin ligands on adjacent cells and mediate contact-dependent bidirectional signaling[1]. Mechanistically, EphA/ephrin-A signaling regulates cell adhesion, positioning, migration, and cytoskeletal organization, linking receptor activation to developmental patterning and adult tissue homeostasis[1][2]. In cancer models, EphA2 shows a key isoform-specific distinction: ephrin-A1 activation inhibits chemotactic migration of glioma and prostate cancer cells, whereas EphA2 overexpression promotes migration in a ligand-independent manner through Akt-dependent Ser897 phosphorylation[3]. Compared with related EphA isoforms, EphA4 is strongly defined by axon-guidance biology, where activated EphA4 recruits α2-chimaerin to mediate growth-cone collapse and neuronal circuit formation[4]. For experimental applications, EphA2 ligands, agonistic antibodies, blocking antibodies, and kinase inhibitors can separate canonical ligand-dependent signaling from noncanonical ligand-independent signaling in cancer-cell migration, invasion, vascular-permeability, and tumor-model studies[3][5][6]. - EphA biology centers on contact-dependent ephrin signaling, cytoskeletal control, and cell-position regulation. - EphA2 research should distinguish ligand-activated suppression from ligand-independent Akt-linked migration. - EphA4 provides a mechanistically distinct axon-guidance model through α2-chimaerin signaling.

EphA Related Products (9):

Cat. No. Product Name Effect Purity
  • HY-133178
    Urolithin D
    		Antagonist 99.72%
    Urolithin D (3,4,8,9-Tetrahydroxy urolithin) is a colonic metabolite of Ellagitannins and a competitive, reversible, and selective antagonist of the EphA receptor. Urolithin D inhibits EphA2-ephrin-A1 binding with an IC50 of 0.9 μM. Urolithin D is also a potent antioxidant that scavenges free radicals and repairs oxidized DNA damage. Additionally, Urolithin D suppresses triglyceride accumulation and promotes fatty acid oxidation by activating the AMPK signaling pathway. Urolithin D can be used for research on tumors, metabolic, and inflammatory diseases.
  • HY-123927
    UniPR1331
    		Inhibitor 98.57%
    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.
  • HY-P11035
    APY-d3
    		Antagonist 99.18%
    APY-d3 is a EphA4-LBD antagonistic peptide with a Kd of 138  nM. APY-d3 is constrained into a bioactive β-hairpin conformation via a head-to-tail disulfide bond. APY-d3 can be used for cancers like gastric and pancreatic cancers and neurodegenerative diseases like amyotrophic lateral sclerosis and Alzheimer’s disease research.
  • HY-P991577
    DS-8895
    		Inhibitor
    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..
  • HY-W078239
    EPHA4 antagonist-1
    		Antagonist
    EPHA4 antagonist-1 (Compound 2) is an EphA4 receptor antagonist. EPHA4 antagonist-1 is also an EphA2 receptor antagonist. EPHA4 antagonist-1 inhibits ephrin-A5 AP binding to EphA4 Fc receptor, with an IC50 of 10 μM.
  • HY-P992403
    MBRC-101 Antibody
    		Inhibitor
    MBRC-101 Antibody is a human monoclonal antibody targeting EphA5. MBRC-101 Antibody can be used to synthesize the ADC MBRC-101.
  • HY-178721
    Lithocholic amide-C2-N(didecane)
    		Inhibitor
    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.
  • HY-P11015
    (123B9)2-Motif
    		Agonist
    (123B9)2-Motif is a selective EphA2 receptor agonist (Kd=4.9 μM) that does not bind to EphA4. (123B9)2-Motif works by inducing EphA2 receptor phosphorylation and oligomerization, thereby promoting receptor activation and internalization. (123B9)2-Motif is primarily used in targeted drug delivery studies for cancers that overexpress EphA2, such as breast cancer, to reduce circulating tumor cells and inhibit metastasis.
  • HY-P11018
    (123B9)2-L2-PTX
    		Agonist
    (123B9)2-L2-PTX is an EphA2-agonistic peptide-drug conjugate (PDC). (123B9)2-L2-PTX consists of a dimeric 123B9 (HY-P10579) and Paclitaxel (HY-B0015). (123B9)2-L2-PTX significantly reduces circulating tumor cells and inhibits lung tumor metastasis in breast-cancer-Metastasis mice model. (123B9)2-L2-PTX can be used for cancers research, such as melanomas and ovarian and breast cancers.