epha4

KYL acetate(676657-00-4 free base) 是EphA4受体酪氨酸激酶抑制剂（Kd = 0.8 μM）；抑制 EphA4-EphrinA5 相互作用 (IC50 = 6.34 μM)。防止 AβO 诱导的突触损伤、树突棘丢失并防止海马 CA3-CA1 传输中 LTP 的阻断。在细胞培养基中表现出较长的半衰期（在 PC3 和 C2C12 培养基中分别为 8 和 12 小时）。它有神经保护作用。

UniPR505 是一种有效的 EphA2 拮抗剂（IC50：0.95 µM），是一种具有抗血管生成作用的新型 3α-氨基甲酰氧基衍生物。

UniPR500为UniPR129的衍生物，属于EphA2受体的竞争性拮抗剂，其Ki为0.78 μM。UniPR500呈现出剂量依赖性，能够减少生物素化Ephrin-A1与EphA2的结合，IC50为1.1 μM。

UniPR129 is a competitive Eph-ephrin antagonist agent that acts by blocking in vitro angiogenesis at low micromolar concentrations.

123C4 是选择性的、竞争性的受体酪氨酸激酶EPHA4激动剂，Ki 为 0.65 μM.

KYL peptide 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.

PSAM (pharmacologically selective actuator module) agonist. Activates PSAML141F-GlyR chimeric ion channels. Inhibits activity of neurons expressing PSAML141F-GlyR in vivo and activates locus coeruleus noradrenergic neurons expressing PSAML141F,Y115F-5-HT3 ion channels. Recommended concentration for use in mice is 5 mg kg or lower. Plasmid vectors for the transfection of cells with PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 are available from Addgene. Lovett-Barron et al (2012) Regulation of neuronal input transformations by tunable dendritic inhibition. Nat.Neurosci. 15 423 PMID:22246433 |Satoh et al (2016) Context-dependent gait choice elicited by EphA4 mutation in Lbx1 spinal interneurons. Neuron 89 1046 PMID:26924434 |Atasoy et al (2012) Deconstruction of a neural circuit for hunger. Nature 488 172 PMID:22801496 |Hirschberg et al (2017) Functional dichotomy in spinal- vs prefrontal-projecting locus coeruleus modules splits descending noradrenergic analgesia from ascending aversion and anxiety in rats. Elife 6 e29808 PMID:29027903

EPHA2 A4 GAK-IN-1 (compound 55) 作为EPHA2 EPHA4和GAK的高效抑制剂,其对EPHA2和GAK的KD值依次为180.5 nM和19.2 nM.该化合物在微粒体中表现出良好的稳定性,预测半衰期达4.6小时.此外,EPHA2 GAK-IN-1显示出显著的抗病毒能力,能有效阻止登革热病毒侵染Huh7肝细胞.

UniPR1454 通过靶向 EphA2 receptor 并阻断 EphA2-ephrin A1 的相互作用来发挥作用,其 IC50 值为 2.6 μM.此外,UniPR1454 能有效抑制胶质母细胞瘤细胞株 U251 的细胞增殖.

123B9 是一种针对肿瘤的归巢剂，具备高效与选择性作为EphA2激动剂，其Kd值为4.0 μM。该化合物专门针对EphA2酪氨酸激酶受体的配体结合域。在最相关的EphA3和EphA4受体配体结合域上，123B9不会产生显著抑制效果。