1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. Ephrin Receptor

Ephrin Receptor (Ephrin受体)

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 相关产品 (10):

目录号 产品名 作用方式 纯度
  • HY-18007
    ALW-II-41-27 Inhibitor 99.70%
    ALW-II-41-27是 Eph 家族酪氨酸激酶抑制剂,抑制Eph2的 IC50为11 nM。
  • HY-13258A
    NVP-BHG712 Inhibitor 99.78%
    NVP-BHG712 是具有口服活性的EphB4 激酶自身磷酸化 的抑制剂,其对EphA2 和EphB4 的 IC50 值分别为 3.3 nM 和 3 nM。
  • HY-13314
    Tesevatinib Inhibitor ≥98.0%
    Tesevatinib (XL-647; EXEL-7647; KD-019) 是口服可用的多靶点酪氨酸激酶抑制剂; 抑制 EGFRErbB2KDRFlt4EphB4 激酶活性的 IC50 值分别为 0.3,16,1.5,8.7,和1.4 nM。
  • HY-13258
    NVP-BHG712 isomer 99.46%
    NVP-BHG712 isomer,是NVP-BHG712 的位置异构体,与EPHA2和EPHB4显示保守非键结合。
  • HY-16265
    JI-101 Inhibitor 99.43%
    JI-101是有口服活性的有抗癌活性的多靶点激酶抑制剂,可抑制 VEGFR2PDGFRβEphB4
  • HY-123607
    UniPR129 Antagonist
    UniPR129 是一种有效但有问题的 Eph/ephrin 拮抗剂。UniPR129 具有研究癌症疾病的潜力。
  • HY-P0177
    123C4 Agonist 99.05%
    123C4 是一种有效、选择性的,竞争性受体酪氨酸激酶 EPHA4 激动剂,Ki 值为 0.65 μM.
  • HY-14979A
    ML786 dihydrochloride Inhibitor
    ML786 dihydrochloride 是一种有效和具有口服活性的 Raf 抑制剂,对 V600EΔB-Rafwt B-RafC-RafIC50 值分别为2.1,4.2 和 2.5 nM。ML786 dihydrochloride 还抑制 Abl-1DDR2EPHA2KDRRET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM)。ML786 dihydrochloride 可用于癌症研究。
  • HY-P2264
    KYL peptide Inhibitor
    KYL peptide 是一种拮抗肽,可选择性靶向 EphA4。KYL peptide 与 EphA4 的配体结合域结合,有效缓解 Aβ 诱导的 AD 小鼠突触功能障碍和突触可塑性缺陷。KYL peptide 可促进损伤后神经再生,调节免疫反应。
  • HY-131005
    Eph inhibitor 2 Inhibitor
    Eph inhibitor 2 (Example 35) 是 Eph 家族酪氨酸激酶抑制剂。
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