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Ephrin Receptor

Eph receptors (Ephs, after erythropoietin-producing human hepatocellular receptors) are a group of receptors that are activated in response to binding with Eph receptor-interacting proteins (Ephrins). Ephs form the largest known subfamily of receptor tyrosine kinases (RTKs). Both Eph receptors and their corresponding ephrin ligands are membrane-bound proteins that require direct cell-cell interactions for Eph receptor activation. Eph/ephrin signaling has been implicated in the regulation of a host of processes critical to embryonic development including axon guidance, formation of tissue boundaries, cell migration, and segmentation. Additionally, Eph/ephrin signaling has recently been identified to play a critical role in the maintenance of several processes during adulthood including long-term potentiation, angiogenesis, and stem cell differentiation and cancer.

AWL-II-38.3
T385111135205-94-5
AWL-II-38.3 is a highly potent EphA3 inhibitor with potent kinase inhibitory activity against EphA3 but no significant cellular activity against Src family kinases or b-raf.
  • $74
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Sitravatinib
T43491123837-84-2
Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.
  • $47
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TargetMol | Citations Cited
ALW-II-41-27
T43441186206-79-0
ALW-II-41-27 (Eph receptor tyrosine kinase inhibitor), an Eph receptor tyrosine kinase inhibitor, is used for cancer therapy.
  • $63
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TargetMol | Inhibitor Sale
ALW-II-49-7
T677361135219-23-6
ALW-II-49-7 is a selective and potent inhibitor of EphB2 kinase, with an EC50 value of 40 nM in cell.
  • $65
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TargetMol | Inhibitor Sale
Urolithin D
T74005131086-98-1
Urolithin D is a competitive and selective reversible antagonist of the EphA receptor, an ellagitannin colonic metabolite that inhibits EphA2 phosphorylation in prostate cancer cells, attenuates triglyceride accumulation in adipocytes and hepatocyte cultures, and may be used in the study of metabolic disorders.
  • $95
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UniPR505
T733682938227-14-4In house
UniPR505 is a potent EphA2 antagonist (IC50: 0.95 µM), a novel 3α-carbamoyloxy derivative with antiangiogenic properties.
  • $518
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Tesevatinib
TQ0166781613-23-8
Tesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor with IC50 values ​​of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4.
  • $109
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NVP-BHG712
T6348940310-85-0
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
  • $31
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Dasatinib monohydrate
T1448L863127-77-9
Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.
  • $33
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TargetMol | Citations Cited
Tivozanib
T2456475108-18-0
Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.
  • $34
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NVP-BHG712 isomer
T194872245892-85-5
NVP-BHG712 isomer shows conserved non-bonded binding to EPHA2 and EPHB4.
  • $36
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123C4
TP15612034159-30-1
123C4 is a potent, selective, and competitive agonist of the receptor tyrosine kinase EPHA4 (Ki=0.65 μM)[1].
  • $147
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TargetMol | Inhibitor Sale
KYL acetate(676657-00-4 free base)
TP1895L1
KYL acetate is an EphA4 receptor tyrosine kinase inhibitor (Kd = 0.8 μM); inhibits EphA4-EphrinA5 interactions (IC50 = 6.34 μM). Prevents AβO induced synaptic damage, dendritic spine loss and prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. Exhibits a long half life in cell culture media (8 and 12 hours in PC3 and C2C12 media respectively). Neuroprotective.
  • $133
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AZ12672857
T9650945396-55-4In house
AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM. AZ12672857 inhibits cell proliferation of Src transfected 3T3 cells with IC50 of 2 nM and autophosphorylation of EphB4 in transfected CHO-K1 cells with IC50 of 9 nM.
  • $64
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Ehp-inhibitor-2
T5452861249-77-6
Ehp-inhibitor-2 is an Eph family tyrosine kinase inhibitor targeting Eph receptors.
  • $39
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Eph inhibitor 2
T5451861249-59-4
Eph inhibitor 2 is an Eph family tyrosine kinase inhibitor targeting Eph receptors.
  • $87
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JI-101
T3476900573-88-8
JI-101 (CGI-1842) is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 (EphB4).
  • $31
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UniPR1447
T808971809170-68-0
UniPR1447 is a dual antagonist for both EphA2 and EphB2 receptors, exhibiting an IC50 value of 6.6 μM against EphA2-ephrin-A1 binding [1].
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8-10 weeks
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UniPR1449
T80896
UniPR1449 is an EphA2 receptor antagonist with a KD of 3.8±2.4 μM, which is significant in cancer pathophysiology [1].
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