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-18007
    ALW-II-41-27
    		Inhibitor 99.33%
    ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.
    ALW-II-41-27
  • HY-13258A
    NVP-BHG712
    		Inhibitor 99.71%
    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-18833
    ALW-II-49-7
    		Inhibitor 99.97%
    ALW-II-49-7 is a selective EphB2 kinase inhibitor with an EC50 value of 40 nM in cell.
    ALW-II-49-7
  • HY-18832
    AWL-II-38.3
    		Inhibitor 99.71%
    AWL-II-38.3 is a potent ephrin-A receptor (EphA3) kinase inhibitor. AWL-II-38.3 does not exhibit significant cellular activity against Src-family kinases nor against b-raf.
    AWL-II-38.3
  • HY-133178
    Urolithin D
    		Antagonist 99.72%
    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
  • HY-185227
    EphB4-IN-1
    		Inhibitor
    EphB4-IN-1 is a selective EphB4 tyrosine kinase inhibitor with IC50 values of 0.16-0.30 μM. EphB4-IN-1 binds to the ATP binding site of EphB4 in a DFG-in conformation, forming four stable intermolecular hydrogen bonds. EphB4-IN-1 also inhibits Src, Abl1, Lck, and EGFR kinases. EphB4-IN-1 inhibits EphB4 autophosphorylation. EphB4-IN-1 can be used for the research of cancer, such as non small cell lung cancer.
    EphB4-IN-1
  • HY-P992403
    MBRC-101 Antibody
    		Inhibitor
    MBRC-101 Antibody is a human monoclonal antibody targeting EphA5. MBRC-101 Antibody can be used to synthesize the ADC MBRC-101.
    MBRC-101 Antibody
  • HY-P991975
    Anti-EphB3 Antibody
    		Inhibitor
    Anti-EphB3 Antibody is an anti-EphB3 antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-EphB3 Antibody
  • HY-107460
    LDN-211904 oxalate
    		Inhibitor 99.0%
    LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC.
    LDN-211904 oxalate
  • HY-P990627
    Anti-EphA2 Antibody (1C1)
    		Inhibitor 99.9%
    Anti-EphA2 Antibody (1C1) (MEDI-547 antibody) is an anti-EphA2 monoclonal antibody. Anti-EphA2 Antibody (1C1) can induce degradation of EphA2 protein. Anti-EphA2 Antibody (1C1) conjugated with McMMAF (HY-15578) can form an antibody-conjugated drugs, which has potent antitumor activity. Anti-EphA2 Antibody (1C1) can be used for the research of cancer, such as prostate cancer and glioma.
    Anti-EphA2 Antibody (1C1)
  • HY-P0177
    123C4
    		Agonist 99.46%
    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
    		99.32%
    NVP-BHG712 isomer, a regioisomer of NVP-BHG712, shows conserved non-bonded binding to EPHA2 and EPHB4.
    NVP-BHG712 isomer
  • HY-16265
    JI-101
    		Inhibitor 98.99%
    JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.
    JI-101
  • HY-123607
    UniPR129
    		Antagonist 99.23%
    UniPR129 is a potent and orally active Eph/ephrin antagonist. UniPR129 can inhibit EphA2-ephrin-A1 interaction with an IC50 of 945 nM and a Ki of 370 nM. UniPR129 can inhibit angiogenesis and show antitumor and neuroprotective effect. UniPR129 can be used for the researches of cancer and neurological disease, such as colorectal cancer and optic neuropathy.
    UniPR129
  • HY-148065
    FMF-06-098-1
    		Inhibitor 98.77%
    FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1.
    FMF-06-098-1
  • HY-114199
    Eph inhibitor 1
    		Inhibitor 99.92%
    Eph inhibitor 1 is a potent Eph inhibitor. Eph inhibitor 1 has the potential for the research of neurological disorders.
    Eph inhibitor 1
  • 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-147637
    EphA2 agonist 1
    		Agonist 98.57%
    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-123927
    UniPR1331
    		Inhibitor 98.57%
    UniPR1331 is an orally active 3β-hydroxy-Δ5-choline acid derivative that inhibits Eph-ephrin interactions. UniPR1331 blocks the interaction of VEGFR2 with its natural ligand vascular endothelial growth factor and inhibits subsequent autophosphorylation, signaling, and pro-angiogenic activation of endothelial cells. UniPR1331 exhibits anti-angiogenesis, anti-cancer and anti-inflammation effects. UniPR1331 can be used for the researches of cancer and inflammation, such as glioma and colitis.
    UniPR1331
  • HY-P3717
    Targefrin
    		99.80%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Ephrin Receptor Isoform Comparison

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