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

Ephrin Receptor

Ephrin Receptor

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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 Isoform Specific Products:

Ephrin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    NVP-BHG712
  • HY-18007
    ALW-II-41-27
    		Inhibitor 99.63%
    ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.
    ALW-II-41-27
  • 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.
    ALW-II-49-7
  • HY-13314
    Tesevatinib
    		Inhibitor 99.21%
    Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, VEGFR2/KDR/Flk-1, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.
    Tesevatinib
  • HY-133178
    Urolithin D
    		Antagonist 99.72%
    Urolithin D is competitive and reversible antagonist of EphA receptors. Urolithin D exhibits intra-classes selectivity.
    Urolithin D
  • HY-P10579
    123B9
    		Agonist
    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.
    123B9
  • 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.
    A11
  • 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.
    EPHA2/A4/GAK-IN-1
  • HY-P0177
    123C4
    		Agonist 99.71%
    123C4 is a potent, selective and competitive agonist of the receptor tyrosine kinase EPHA4, with a Ki value of 0.65 μM.
    123C4
  • HY-13258
    NVP-BHG712 isomer
    		99.58%
    NVP-BHG712 isomer, a regioisomer of NVP-BHG712, shows conserved non-bonded binding to EPHA2 and EPHB4.
    NVP-BHG712 isomer
  • HY-107460
    LDN-211904 oxalate
    		Inhibitor ≥99.0%
    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.
    LDN-211904 oxalate
  • HY-123607
    UniPR129
    		Antagonist 99.23%
    UniPR129 is a potent Eph/ephrin antagonist with IC50s of 0.84-3.01 μM. UniPR129 has the potential for the research of cancer disease.
    UniPR129
  • HY-P99655
    Ifabotuzumab
    		Inhibitor
    Ifabotuzumab (KB004) is an IgG1κ antibody targeting EphA3 (KD=610 pM). Ifabotuzumab induces tumor cell apoptosis, activates Antibody-dependent cell mediated cytotoxicity (ADCC), and damages tumor vasculature. Ifabotuzumab reduces human idiopathic pulmonary fibrosis (IPF) CCR10+ cells and improves pulmonary fibrosis.
    Ifabotuzumab
  • HY-16265
    JI-101
    		Inhibitor 99.78%
    JI-101 is an orally available multi-kinase inhibitor of VEGFR2/KDR/Flk-1, PDGFRβ and EphB4 with potent anti-cancer activity.
    JI-101
  • 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.
    EphA2 agonist 1
  • HY-114199
    Eph inhibitor 1
    		Inhibitor 98.04%
    Eph inhibitor 1 is a potent Eph inhibitor. Eph inhibitor 1 has the potential for the research of neurological disorders.
    Eph inhibitor 1
  • HY-P2264
    KYL peptide
    		Inhibitor 99.09%
    KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). 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.
    KYL peptide
  • HY-P3717
    Targefrin
    		99.45%
    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.
    Targefrin
  • HY-157019
    UniPR1447
    		Antagonist
    UniPR1447 is Dual EphA2 and EphB2 antagonist, with an IC50 of 6.6 μM for EphA2−ephrin-A1 binding.
    UniPR1447
  • 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.
    SA-VA
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Ephrin Receptor Isoform Comparison

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