2. Protein Tyrosine Kinase/RTK
  3. Ephrin Receptor

Ephrin Receptor

The Eph receptor tyrosine kinase (RTK) family comprises the largest group of surface receptors and are categorized into EphA or EphB subclasses based on sequence homology and preferential binding to their ephrin-A and ephrin-B ligands, respectively.

In humans, nine EphA (EphA1-8,10) and five EphB (EphB1-4,6) receptors are expressed, along with five ephrin-A and three ephrin-B ligands. Unlike most RTKs, Eph receptors interact with ligands that are often membrane-bound, allowing both “forward signaling” in the receptor-bound cell and “reverse signaling” in the ephrin-bound cell. In addition to “forward signaling,” Eph receptors can signal in the absence of ligand binding and kinase activation through cross-talk with other RTKs, such as HER2.

Eph receptor tyrosine kinases and their ligands, the ephrins, play key roles in the regulation of migration and cell adhesion during development, thereby influencing cell fate, morphogenesis and organogenesis. By now, many Eph receptors and ephrins have also been found to play important roles in the progression of cancer. Therefore, the Eph/ephrin system is considered a promising therapeutic target.

Ephrin Receptor Related Products (36):

Cat. No. Product Name Effect Purity
  • HY-18832
    AWL-II-38.3 Inhibitor 99.71%
    AWL-II-38.3 is a potent ephrin-A receptor (EphA3) kinase inhibitor. AWL-II-38.3 does not exhibit significant cellular activity against Src-family kinases nor against b-raf[1][2][1][2].
  • HY-13258A
    NVP-BHG712 Inhibitor 99.70%
    NVP-BHG712 is an oral active EphB4 kinase autophosphorylation inhibitor, with IC50 values of 3.3 nM and 3.0 nM for EphA2 and EphB4, respectively[1][2].
  • HY-18007
    ALW-II-41-27 Inhibitor 99.38%
    ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.
  • HY-133178
    Urolithin D Antagonist 99.72%
    Urolithin D is competitive and reversible antagonist of EphA receptors. Urolithin D exhibits intra-classes selectivity[1].
  • HY-18833
    ALW-II-49-7 Inhibitor 99.80%
    ALW-II-49-7 is a selective EphB2 kinase inhibitor with an EC50 value of 40 nM in cell[1].
  • HY-133178R
    Urolithin D (Standard) Antagonist
    Azathramycin (Standard) is the analytical standard of Azathramycin. This product is intended for research and analytical applications. Azathramycin (Azaerythromycin A) is an antibiotic that targets ribosomes and possesses antibacterial activity, which can be used in research related to infectious diseases[1].
  • HY-171175
    UniPR500 Antagonist
    UniPR500, a UniPR129 derivative, is a competitive EphA2 receptor antagonist with a Ki of 0.78 μM. UniPR500 dose-dependently reduces binding of biotinylated ephrin-A1 to EphA2 with an IC50 value of 1.1 μM[1].
  • HY-171217
    TG-100435 Inhibitor
    TG-100435 is a multitargeted, orally active protein tyrosine kinase inhibitor, with Ki of 13 to 64 nM for Src, Lyn, Abl, Yes, Lck, and EphB4. TG-100435 plays an important role in cancer research[1].
  • HY-P990627
    Anti-EphA2 Antibody (1C1)
    Anti-EphA2 Antibody (1C1) (MEDI-547 antibody) is a humanized antibody expressed in CHO cells, targeting EphA2. Anti-EphA2 Antibody (1C1) contains huIgG1 type heavy chain and huκ type light chain, with a predicted molecular weight (MW) of 146.68 kDa. The isotype control for Anti-EphA2 Antibody (1C1) can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
  • HY-147637
    EphA2 agonist 1 Agonist 99.32%
    EphA2 agonist 1 (Compound 7bg) is a potent EphA2 receptor agonist. EphA2 agonist 1 shows great potency and selectivity toward EphA2 overexpressed glioblastoma cells and stimulates EphA2 phosphorylation[1].
  • HY-P0177
    123C4 Agonist 99.83%
    123C4 is a potent, selective and competitive agonist of the receptor tyrosine kinase EPHA4, with a Ki value of 0.65 μM[1].
  • HY-13258
    NVP-BHG712 isomer 99.58%
    NVP-BHG712 isomer, a regioisomer of NVP-BHG712, shows conserved non-bonded binding to EPHA2 and EPHB4[1].
  • HY-P990405
    Anti-EphB2 Antibody Inhibitor
    The Anti-EphB2 Antibody is a CHO expressed human antibody that targets EphB2. The Anti-EphB2 Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-EphB2 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
  • HY-157019
    UniPR1447 Antagonist 99.46%
    UniPR1447 is Dual EphA2 and EphB2 antagonist, with an IC50 of 6.6 μM for EphA2−ephrin-A1 binding[1].
  • HY-170517
    PKMYT1-IN-8 Inhibitor
    PKMYT1-IN-8 (Compound 137) is the inhibitor for PKMYT1 with an IC50 of 9 nM. PKMYT1-IN-8 inhibits EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2with IC50s of 1.79, 3.17, 4.29, 6.32, 6.83, 8.10, and 10.9 μM, respectively. PKMYT1-IN-8 inhibits the proliferation of cancer cell OVCAR3 with GI50 of 2.02 μM[1].
  • HY-P10579
    123B9 Agonist 99.67%
    123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a Kd value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors[1].
  • HY-P10412
    A11 Inhibitor
    A11 (ANXA1-derived 11 amino acid–long peptide) is an ANXA1-EphA2 interaction blocker peptide. A11 decreases ANXA1 bound to EphA2 and increased Cbl (an E3 ubiquitin ligase of EphA2) bound to EphA2. A11 efficiently decreases EphA2 level, and substantially increases EphA2 ubiquitination. A11 increases EphA2 internalization and colocalization of EphA2 and Cbl in the NPC cells. A11 inhibits nasopharyngeal carcinoma (NPC) cell proliferation, migration and invasion. A11 inhibits angiogenesis[1].
  • HY-155685
    SA-VA Inhibitor
    SA-VA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase[1].
  • HY-159174
    EPHA2/A4/GAK-IN-1 Inhibitor
    EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with KD values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. EPHA2/GAK-IN-1 shows an extrapolated half-life time of 4.6 h in a microsomal stability assay. EPHA2/GAK-IN-1 shows antiviral activity and prevents dengue virus infection of Huh7 liver cells[1].
  • HY-161171
    Antimalarial agent 37 Inhibitor
    Antimalarial agent 37 (compound 33) is a selective inhibitor against Type Ⅱ kinase with antiplasmodial activity. Antimalarial agent 37 exhibited cytotoxicity and selectivity towards cancer cells HepG2 and MCF 7[1].