- Signaling Pathways
- Protein Tyrosine Kinase/RTK
- Ephrin Receptor
Ephrin Receptor
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
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Ephrin Receptor Related Products (62)
Related Products (62)
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Recombinant Proteins (86)
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Antibodies (8)
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Ephrin Receptor Isoform Comparison
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Antimalarial agent 37
0 ImagesCat. No.: HY-161171CAS No.: 2982633-16-7Antimalarial 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. -
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Nastorazepide hemicalcium
0 ImagesCat. No.: HY-14575CAS No.: 343326-69-2Synonyms: Z-360 hemicalciumNastorazepide (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. -
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ML786 dihydrochloride
0 ImagesCat. No.: HY-14979ACAS No.: 1237536-18-3ML786 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. -
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Anti-Ephrin-B2 Antibody
0 ImagesCat. No.: HY-P991965 -
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(123B9)2-L2-PTX
0 ImagesCat. No.: HY-P11018(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. -
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SA-PA
0 ImagesCat. No.: HY-155684CAS No.: 3058085-76-7SA-PA is an intracellular self-assembling CRBN-recruiting PROTAC composed of an alkynylated Sorafenib precursor (SA) and an azidated Pomalidomide precursor (PA). SA-PA promotes the ubiquitination and proteasomal degradation of VEGFR-2, EphB4, and PDGFR-β, and exhibits inhibitory activity against U87 and A549 cell proliferation. SA-PA is used in cancer-related research, such as glioblastoma and non-small cell lung cancer. -
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Lithocholic amide-C2-N(didecane)
0 ImagesCat. No.: HY-178721CAS No.: 2768690-22-6Lithocholic 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. -
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JI-101 hydrochloride
0 ImagesCat. No.: HY-16265ACAS No.: 2514957-81-2JI-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. -
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- UniPR1449
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UniPR1454
0 ImagesCat. No.: HY-163835UniPR1454 targets EphA2 receptor, inhibits the EphA2-ephrin A1 interaction with an IC50 of 2.6 μM. UniPR1454 inhibits the proliferation of glioblastoma cell U251. -
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EphB4-IN-2
0 ImagesCat. No.: HY-10654CAS No.: 1192216-03-7EphB4-IN-2 is a tyrosine kinase inhibitor targeting the Eph family and Src family. EphB4-IN-2 binds to the ATP-binding site of the kinase domain of EphB4, and exhibits high affinity for tyrosine kinases with threonine as the gatekeeper residue, such as Abl, Lck and Src. EphB4-IN-2 can be used in research related to tumor-associated angiogenesis. -
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LY2457546
0 ImagesCat. No.: HY-107144CAS No.: 908265-94-1LY2457546 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. -
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- EphA2 agonist 2
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ML786
0 ImagesCat. No.: HY-14979CAS No.: 1237586-97-8 -
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Multi-kinase-IN-12
0 ImagesCat. No.: HY-18692CAS No.: 597544-21-3Multi-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. -
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- EphA4 agonist compound 23
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EPHB4 modulator-1
0 ImagesCat. No.: HY-186005CAS No.: 633281-74-0 -
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- UniPR500
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LDN-211904 oxalate (Standard)
0 ImagesCat. No.: HY-107460RCAS No.: 1198408-78-4LDN-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. -
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- TG-100435
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