The majority of surface receptors belong to the Eph receptor tyrosine kinase (RTK) family, which is divided into EphA and EphB subclasses based on sequence homology and preferential binding to ephrin-A and ephrin-B ligands, respectively.
Ephrin-A and Ephrin-B ligands, as well as nine EphA (EphA1-8,10) and five EphB (EphB1-4,6) receptors, are expressed in humans. Eph receptors interact with ligands that are frequently membrane-bound, which makes them different from most RTKs and enables both "forward signaling" in the receptor-bound cell and "reverse signaling" in the ephrin-bound cell. Eph receptors can signal in the absence of ligand binding and kinase activation in addition to "forward signaling" by interacting with other RTKs, such as HER2.
In order to control migration and cell adhesion during development, eph receptor tyrosine kinases and their ligands, the ephrins, have a major impact on cell fate, morphogenesis, and organogenesis. Ephrins and numerous Eph receptors have now also been discovered to play significant roles in the development of cancer. Consequently, it is thought that the Eph/ephrin system represents a promising therapeutic target.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V121268 | (123B9)2-L2-PTX | (123B9)2-L2-PTX is an EphA2 agonist peptide-drug conjugate (PDC). | |
|
V121269 | (123B9)2-Motif | (123B9)2-Motif is a selective EphA2 receptor agonist (Kd=4.9 μM) that does not bind to EphA4. | |
|
V88023 | 123B9 | 2225868-19-7 | 123B9 is a tumor homing agent and a potent and selective EphA2 agonist with a Kd of 4.0 μM. |
|
V115444 | 150D4 | 2866306-73-0 | 150D4 is a potent, selective EphA4 agonist that can cross the blood-brain barrier. |
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V88021 | A11 | 2412926-29-3 | A11 (ANXA1-derived 11 amino acid–long peptide) is an ANXA1-EphA2 interaction blocking peptide. |
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V127958 | A11 acetate | A11 acetate is an ANXA1-EphA2 interaction blocking peptide. | |
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V8240 | ALW-II-41-27 | 1186206-79-0 | ALW-II-41-27 is a potent Eph receptor tyrosine kinase inhibitor withIC50 of 11 nM for Eph2. |
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V120271 | APY-d3 | APY-d3 is an EphA4-LBD antagonistic peptide with a Kd value of 138 nM. | |
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V134372 | DS-8895 | DS-8895 is an anti-EphA2 monoclonal antibody that specifically binds to the EphA2 receptor and cells expressing EphA2. | |
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V69448 | Eph inhibitor 2 | 861249-59-4 | Eph inhibitor 2 (Example 35) is an Eph family tyrosine kinase inhibitor (TKI). |
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V104827 | EphA2 antagonist 1 | 1428095-28-6 | EphA2 antagonist 1 (4b) is a bile acid derivative and epidermal growth factor receptor 2 (EPHA2) inhibitor. |
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V101118 | EPHA2/A4/GAK-IN-1 | EPHA2/A4/GAK-IN-1 (Compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with KD values of 180.5 nM and 19.2 nM for EPHA2 and GAK, respectively. | |
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V115629 | EphA4 agonist compound 23 | EphA4 agonist compound 23 is a novel EphA4 agonist peptide mimic. | |
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V113893 | EPHA4 antagonist-1 | 313701-92-7 | EPHA4 antagonist-1 (compound 2) is an EphA4 receptor antagonist. |
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V110451 | EPHB4 modulator-1 | 633281-74-0 | EPHB4 Regulator-1 is a regulator of EPHB4. |
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V135154 | EphB4-IN-2 | 1192216-03-7 | EphB4-IN-2 is a tyrosine kinase inhibitor with an IC50 value of 1.6 nM for human EphB4 and is selective for kinases containing threonine-gated residues. |
|
V2827 | JI-101 | 900573-88-8 | JI-101 is an orally bioactive multi-kinase inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRb), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities. |
|
V69446 | KYL peptide | 676657-00-4 | KYL peptide is an antagonist peptide that selectively targets EphA4. |
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V88022 | LDN-211904 | 1198408-39-7 | LDN-211904 is an inhibitor of EphB3 receptor tyrosine kinase. |
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V111063 | Lithocholic amide-C2-N(didecane) | 2768690-22-6 | Lithocholamide-C2-N(didecane) (compound LC10) is an analogue of lithocholic acid. |