EphA4 receptor tyrosine kinase inhibitor (Kd = 0.8 μM), which 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. It shows neuroprotective effect.
CAT No: R0975
CAS No:676657-00-4
Synonyms/Alias:676657-00-4;KYL peptide;L-Leucine,L-lysyl-L-tyrosyl-L-leucyl-L-prolyl-L-tyrosyl-L-tryptophyl-L-prolyl-L-valyl-L-leucyl-L-seryl-L-seryl-;KYL (trifluoroacetate salt);KYL;KYL TFA;HY-P2264;AKOS025142078;DA-54717;CS-0120761;G15846;
KYL was also shown to prevent growth cone collapse in chicken retinal explants and dissociated cultures of rat cortical neurons, promote nerve regeneration and functional recovery in a rat model of spinal cord injury, and inhibit the adhesion of human T-cells to endothelial cells. Thus, KYL can target human, mouse, rat and chicken EphA4 and may be useful for promoting nerve regeneration after injury and modulating immune responses.
Distinctive Binding of Three Antagonistic Peptides to the Ephrin-Binding Pocket of the EphA4 Receptor
STI and KYL inhibitors prevented AβO-induced dendritic spine loss. Although the absence of EphA4 did not completely rescue the dendritic spine loss, EphA4-knockout neurons show a significant decrease in AβO-induced dendritic spine loss. Furthermore, protection was observed in mature neurons (with established synapses) transfected with either c-Abl shRNA or EphA4 shRNA.
EphA4 activation of c-Abl mediates synaptic loss and LTP blockade caused by amyloid-β oligomers
2. TMEM16F and dynamins control expansive plasma membrane reservoirs
3. Autoinhibition and phosphorylation-induced activation of phospholipase C-γ isozymes
5. Cationic cell-penetrating peptides are potent furin inhibitors
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