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-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 (Pink: target protein ligand (HY-169396); Blue: VHL ligand (HY-112078); Black: Linker (HY-124380)).
    FMF-06-098-1
  • HY-170517
    PKMYT1-IN-8
    		Inhibitor 99.31%
    PKMYT1-IN-8 (Compound 137) is the inhibitor for PKMYT1 with an IC50 of 9 nM. PKMYT1-IN-8 inhibits EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2with IC50s of 1.79, 3.17, 4.29, 6.32, 6.83, 8.10, and 10.9 μM, respectively. PKMYT1-IN-8 inhibits the proliferation of cancer cell OVCAR3 with GI50 of 2.02 μM.
    PKMYT1-IN-8
  • HY-157019
    UniPR1447
    		Antagonist 99.46%
    UniPR1447 is Dual EphA2 and EphB2 antagonist, with an IC50 of 6.6 μM for EphA2−ephrin-A1 binding.
    UniPR1447
  • HY-P10579
    123B9
    		Agonist 99.67%
    123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a Kd value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors.
    123B9
  • HY-P10412
    A11
    		Inhibitor 98.49%
    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-146375
    UniPR505
    		Antagonist 98.23%
    UniPR505 (Compound 14) is an EphA2 antagonist with an IC50 of 0.95 µM. UniPR505 displays anti-angiogenic properties.
    UniPR505
  • HY-131005
    Eph inhibitor 2
    		Inhibitor
    Eph inhibitor 2 (Example 35) is a Eph family tyrosine kinase inhibitor.
    Eph inhibitor 2
  • 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-133178R
    Urolithin D (Standard)
    		Antagonist
    Urolithin D (Standard) (3,4,8,9-Tetrahydroxy urolithin (Standard)) is the analytical standard of Urolithin D (HY-133178). This product is intended for research and analytical applications. 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 (Standard)
  • 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-14575
    Nastorazepide hemicalcium
    		Inhibitor
    Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide hemicalcium
  • HY-P10960
    Nuzefatide
    		Ligand
    Nuzefatide is an ephrin receptor binding peptide.
    Nuzefatide
  • 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-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-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-P11035
    APY-d3
    		Antagonist
    APY-d3 is a EphA4-LBD antagonistic peptide with a Kd of 138  nM. APY-d3 is constrained into a bioactive β-hairpin conformation via a head-to-tail disulfide bond. APY-d3 can be used for cancers like gastric and pancreatic cancers and neurodegenerative diseases like amyotrophic lateral sclerosis and Alzheimer’s disease research.
    APY-d3
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Ephrin Receptor Isoform Comparison

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