2. Protein Tyrosine Kinase/RTK
  3. Ephrin Receptor

Ephrin Receptor

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 Related Products (18):

Cat. No. Product Name Effect Purity
  • HY-13258
    NVP-BHG712 isomer 99.46%
    NVP-BHG712 isomer, a regioisomer of NVP-BHG712, shows conserved non-bonded binding to EPHA2 and EPHB4[1].
  • HY-13314
    Tesevatinib Inhibitor
    Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.
  • HY-13258A
    NVP-BHG712 Inhibitor 99.78%
    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[1][2].
  • HY-16265
    JI-101 Inhibitor 99.43%
    JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.
  • 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.
  • 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[1][2].
  • HY-P3717
    Targefrin
    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[1].
  • HY-18833
    ALW-II-49-7 Inhibitor
    ALW-II-49-7 is a selective EphB2 kinase inhibitor with an EC50 value of 40 nM in cell[1].
  • HY-147637
    EphA2 agonist 1 Agonist
    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[1].
  • HY-P0177
    123C4 Agonist 99.05%
    123C4 is a potent, selective and competitive agonist of the receptor tyrosine kinase EPHA4, with a Ki value of 0.65 μM[1].
  • HY-148101
    BT5528 Activator
    BT5528 is a bicyclic peptide toxin conjugate, an EphA2 activator. BT5528, made up of a bicyclic peptide and Auristatin E (HY-15582), is derivated from BCY6099. BT5528 shows potent anti-tumor activity without bleeding or coagulation toxicity in rats model[1][2].
  • 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, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers[1].
  • HY-146375
    UniPR505 Antagonist
    UniPR505 (Compound 14) is an EphA2 antagonist with an IC50 of 0.95 µM. UniPR505 displays anti-angiogenic properties[1].
  • HY-131005
    Eph inhibitor 2 Inhibitor
    Eph inhibitor 2 (Example 35) is a Eph family tyrosine kinase inhibitor.
  • 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[1].
  • HY-123607
    UniPR129 Antagonist 99.13%
    UniPR129 is a potent Eph/ephrin antagonist. UniPR129 has the potential for the research of cancer disease[1].
  • HY-P2264
    KYL peptide Inhibitor
    KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor. 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[1][2].
  • HY-107460
    LDN-211904 oxalate Inhibitor
    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[1][2].