1. Signaling Pathways
  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.

Cat. No. Product Name Effect Purity
  • HY-18007
    Inhibitor 99.63%
    ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.
  • HY-13258A
    Inhibitor 99.78%
    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.
  • HY-13314
    Inhibitor 99.21%
    Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.
  • HY-13258
    NVP-BHG712 isomer
    NVP-BHG712 isomer, a regioisomer of NVP-BHG712, shows conserved non-bonded binding to EPHA2 and EPHB4.
  • HY-16265
    Inhibitor 99.43%
    JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.
  • HY-148101
    BT5528 is a bicyclic peptide toxin conjugate, an EphA2 activator. BT5528, made up of a bicyclic peptide and Auristatin E (HY-15582), is derivated from BCY6099. BT5528 shows potent anti-tumor activity without bleeding or coagulation toxicity in rats model.
  • HY-147637
    EphA2 agonist 1
    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.
  • HY-146375
    UniPR505 (Compound 14) is an EphA2 antagonist with an IC50 of 0.95 µM. UniPR505 displays anti-angiogenic properties.
  • HY-P0177
    Agonist 99.05%
    123C4 is a potent, selective and competitive agonist of the receptor tyrosine kinase EPHA4, with a Ki value of 0.65 μM.
  • HY-123607
    Antagonist 99.13%
    UniPR129 is a potent Eph/ephrin antagonist. UniPR129 has the potential for the research of cancer disease.
  • HY-14979A
    ML786 dihydrochloride
    ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.
  • HY-131005
    Eph inhibitor 2
    Eph inhibitor 2 (Example 35) is a Eph family tyrosine kinase inhibitor.
  • HY-P3717
    Targefrin is a potent EphA2-targeting agent, acts as an antagonist. Targefrin binds EphA2-LBD with 21 nM dissociation constant and an IC50 value of 10.8 nM. Targefrin induces cellular receptor internalization and degradation in several pancreatic cancer cell lines.
  • HY-146141
    EphA2 agonist 2
    EphA2 agonist 2 (Lead compound) is a selective EphA2 agonist with antitumor activities. EphA2 agonist 2 can cross the BBB.
  • HY-P2264
    KYL peptide
    KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor. KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses.
  • HY-107460
    LDN-211904 oxalate
    LDN-211904 oxalate (compound 32) is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with cetuximab could be effective in inhibiting STAT3-activated CSC stemness and cetuximab resistance in CRC.
Cat. No. Product Name / Synonyms Species Source