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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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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V69448 | Eph inhibitor 2 | 861249-59-4 | Eph inhibitor 2 (Example 35) is an Eph family tyrosine kinase inhibitor (TKI). |
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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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V81514 | Targefrin | Targefrin is a potent agent that targets EphA2 and works as an antagonist. | |
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V69447 | UniPR1447 | 1809170-68-0 | UniPR1447 is Dual EphA2 and EphB2 antagonist, with IC50 of 6.6 μM for EphA2−ephrin-A1 binding. |
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V81672 | UniPR1449 | UniPR1449 is an EphA2 receptor blocker (antagonist) with Kd of 3.8±2.4 μM and plays important roles in cancer. | |
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V69445 | UniPR505 | 2938227-14-4 | UniPR505 (Compound 14) is an EphA2 antagonist (inhibitor) with IC50 of 0.95 µM. |
|
V69444 | Urolithin D | 131086-98-1 | Urolithin D is a competitive and reversible antagonist of the EphA receptor. |
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