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-P10412
    A11
    		Inhibitor 98.49%
    A11 (ANXA1-derived 11 amino acid-long peptide) is a ANXA1-EphA2 interaction-blocking peptide. A11 reduces ANXA1 bound to EphA2 and increases Cbl (the E3 ubiquitin ligase of EphA2) bound to EphA2. A11 inhibits the proliferation, migration and invasion of nasopharyngeal carcinoma cells. A11 inhibits angiogenesis. A11 can be used in studies related to nasopharyngeal carcinoma.
    A11
  • HY-P2264
    KYL peptide
    		Inhibitor 99.65%
    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-17617
    Nastorazepide
    		Inhibitor 99.95%
    Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide
  • HY-P990405
    Anti-EphB2 Antibody
    		Inhibitor 99.36%
    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).
    Anti-EphB2 Antibody
  • HY-170517
    PKMYT1-IN-8
    		Inhibitor 99.31%
    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.
    PKMYT1-IN-8
  • HY-131005
    Eph inhibitor 2
    		Inhibitor 99.00%
    Eph inhibitor 2 (Example 35) is a Eph family tyrosine kinase inhibitor.
    Eph inhibitor 2
  • 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.
    APY-d3
  • 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..
    DS-8895
  • 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.
    UniPR1447
  • 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.
    123B9
  • HY-146375
    UniPR505
    		Antagonist 99.68%
    UniPR505 (Compound 14) is an EphA2 antagonist with an IC50 of 0.95 µM. UniPR505 displays anti-angiogenic properties.
    UniPR505
  • 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.
    EPHA4 antagonist-1
  • HY-P11244
    150D4
    		Agonist
    150D4 is an efficient, selective, and blood-brain barrier penetrable EphA4 agonist. 150D4 has excitatory activity and neuroprotective effects. 150D4 can be used for research on neurological conditions.
    150D4
  • 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.
    (123B9)2-Motif
  • 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
  • HY-P10412A
    A11 acetate
    		Inhibitor 98.48%
    A11 (ANXA1-derived 11 amino acid-long peptide) acetate is a ANXA1-EphA2 interaction-blocking peptide. A11 acetate reduces ANXA1 bound to EphA2 and increases Cbl (the E3 ubiquitin ligase of EphA2) bound to EphA2. A11 acetate inhibits the proliferation, migration and invasion of nasopharyngeal carcinoma cells. A11 acetate inhibits angiogenesis. A11 acetate can be used in studies related to nasopharyngeal carcinoma.
    A11 acetate
  • HY-133178R
    Urolithin D (Standard)
    		Antagonist
    Urolithin D (Standard) (3,4,8,9-Tetrahydroxy urolithin (Standard)) is the analytical standard of Urolithin D (HY-133178). This product is intended for research and analytical applications. 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.
    Urolithin D (Standard)
  • 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-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.
    Antimalarial agent 37
  • HY-14575
    Nastorazepide hemicalcium
    		Inhibitor
    Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide hemicalcium
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Ephrin Receptor Isoform Comparison

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