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-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-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-14979A
    ML786 dihydrochloride
    		Inhibitor
    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, VEGFR2/KDR/Flk-1, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.
    ML786 dihydrochloride
  • HY-146375
    UniPR505
    		Antagonist
    UniPR505 (Compound 14) is an EphA2 antagonist with an IC50 of 0.95 µM. UniPR505 displays anti-angiogenic properties.
    UniPR505
  • HY-155684
    SA-PA
    		Inhibitor
    SA-PA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues.
    SA-PA
  • HY-131005
    Eph inhibitor 2
    		Inhibitor
    Eph inhibitor 2 (Example 35) is a Eph family tyrosine kinase inhibitor.
    Eph inhibitor 2
  • HY-157020
    UniPR1449
    		Antagonist
    UniPR1449 is an antagonist of EphA2 receptor, with th KD of 3.8±2.4 μM, that plays an important role in cancer.
    UniPR1449
  • HY-146141
    EphA2 agonist 2
    		Agonist
    EphA2 agonist 2 (Lead compound) is a selective EphA2 agonist with antitumor activities. EphA2 agonist 2 can cross the BBB.
    EphA2 agonist 2
  • HY-136358
    LDN-211904
    		Inhibitor
    LDN-211904 is an inhibitor of EphB3 receptor tyrosine kinase. LDN-211904 enhances the inhibitory activity of EphB3 kinase by maintaining the 2-chloroaniline group and introducing a phenyl or small electron donor substituent to the 5 position of pyrazole and [1,5-a] pyridine. LDN-211904 can be used as a molecular probe to study the function and signaling pathways of EphB3 receptors, especially in the nervous system during neurodevelopment and adulthood.
    LDN-211904
  • HY-14979
    ML786
    		Inhibitor
    ML786 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 also inhibits Abl-1, DDR2, EPHA2, VEGFR2/KDR/Flk-1, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers.
    ML786
  • HY-169849
    EphA2 antagonist 1
    		Inhibitor
    EphA2 antagonist 1 (4b) is a bile acid conjugate and an ephrin type-A receptor 2 (EPHA2) inhibitor.
    EphA2 antagonist 1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Ephrin Receptor Isoform Comparison

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