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-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.
    ML786 dihydrochloride
  • HY-P991965
    Anti-Ephrin-B2 Antibody
    		Inhibitor
    Anti-Ephrin-B2 Antibody is an anti-Ephrin-B2 antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-Ephrin-B2 Antibody
  • HY-P11018
    (123B9)2-L2-PTX
    		Agonist
    (123B9)2-L2-PTX is an EphA2-agonistic peptide-drug conjugate (PDC). (123B9)2-L2-PTX consists of a dimeric 123B9 (HY-P10579) and Paclitaxel (HY-B0015). (123B9)2-L2-PTX significantly reduces circulating tumor cells and inhibits lung tumor metastasis in breast-cancer-Metastasis mice model. (123B9)2-L2-PTX can be used for cancers research, such as melanomas and ovarian and breast cancers.
    (123B9)2-L2-PTX
  • 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-178721
    Lithocholic amide-C2-N(didecane)
    		Inhibitor
    Lithocholic amide-C2-N(didecane) (Compound LC10) is a Lithocholic acid (HY-B0172) analogue. Lithocholic amide-C2-N(didecane) can form lipid nanoparticles spontaneously in the aqueous milieu, permeate through the skin, penetrate the deeper dermal layers, and exert anti-inflammatory effects against psoriasis-like chronic skin inflammations. Lithocholic amide-C2-N(didecane) can inhibit abnormal proliferation of keratinocytes, downregulate the mRNA expression of the psoriasis-associated receptor EphA2 and reduce serum levels of multiple pro-inflammatory factors such as IL-1α, IL-1β, and IFN-γ by inhibiting activation of the Th17/Th2 inflammatory pathway.
    Lithocholic amide-C2-N(didecane)
  • HY-16265A
    JI-101 hydrochloride
    		Inhibitor
    JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity.JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis.JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes.JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route.JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors.
    JI-101 hydrochloride
  • 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-10654
    EphB4-IN-2
    		Inhibitor
    EphB4-IN-2 (compound 66) is a tyrosine kinase inhibitor with an IC50 value of 1.6 nM against human EphB4, and exhibits selectivity toward kinases bearing threonine gatekeeper residues. EphB4-IN-2 also has high ligand efficiency.
    EphB4-IN-2
  • HY-107144
    LY2457546
    		Inhibitor
    LY2457546 is a potent and orally active multi-targeted anti-angiogenic tyrosine kinases inhibitor. LY2457546 demonstrates potent activity against targets that include VEGFR2, PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. LY2457546 can be used for the research of cancer, such as leukemia.
    LY2457546
  • HY-146141
    EphA2 agonist 2
    		Agonist 98.64%
    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-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, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers.
    ML786
  • HY-P991974
    Anti-EPHA4 Antibody
    		Inhibitor
    Anti-EPHA4 Antibody is an anti-EPHA4 antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-EPHA4 Antibody
  • HY-18692
    Multi-kinase-IN-12
    		Inhibitor
    Multi-kinase-IN-12 is a non-selective multi-target inhibitor, with IC50 values against human targets as follows: Flt3 < 0.001 μM, c-Src 0.002 μM, KDR 0.004 μM, Eph-A2, MNK-1 and Flt1 0.011 μM, Lck 0.016 μM, Rsk1 0.21 μM, and α2 subunit of AMPK 0.041 μM. Multi-kinase-IN-12 can be used in research related to solid tumors.
    Multi-kinase-IN-12
  • HY-P11243
    EphA4 agonist compound 23
    		Agonist
    EphA4 agonist compound 23 is a novel EphA4 agonist peptide mimic. EphA4 agonist compound 23 exhibits high affinity, high selectivity, and significant receptor activation ability. EphA4 agonist compound 23 is commonly used in the study of neurodegenerative diseases.
    EphA4 agonist compound 23
  • HY-186005
    EPHB4 modulator-1
    EPHB4 modulator-1 is a EPHB4 modulator.
    EPHB4 modulator-1
  • 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-107460R
    LDN-211904 oxalate (Standard)
    		Inhibitor
    LDN-211904 oxalate (Standard) is the analytical standard of LDN-211904 (oxalate) (HY-107460). This product is intended for research and analytical applications. 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 (Standard)
  • 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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