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-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
  • 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).
    Anti-EphB2 Antibody
  • 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-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-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-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-163835
    UniPR1454
    		Antagonist
    UniPR1454 targets EphA2 receptor, inhibits the EphA2-ephrin A1 interaction with an IC50 of 2.6 μM. UniPR1454 inhibits the proliferation of glioblastoma cell U251.
    UniPR1454
  • 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 a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 shows good metabolic stability in mouse liver microsomes. LDN-211904 with cetuximab could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab (HY-P9905) resistance in CRC.
    LDN-211904
  • 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.
    UniPR500
  • 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.
    TG-100435
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Ephrin Receptor Isoform Comparison

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