Eph A8 Inhibitors
Ephrin receptors (Ephs) are a unique subset of the receptor tyrosine kinase (RTK) family, integral in various cellular processes like cellular migration, adhesion, and positioning. Of the various ephrin receptors, EphA8 stands out for its distinctive biochemical and biophysical characteristics. Eph A8 inhibitors, as the name suggests, are chemical entities designed to specifically block the function of the EphA8 receptor. The inhibition usually works by preventing the phosphorylation, a key post-translational modification, of the receptor, thus disrupting its signaling pathways.
The chemical structures of Eph A8 inhibitors can vary widely, and their exact mechanism of action often relies on their structural intricacies. Some inhibitors act by competing with the ATP-binding pocket of the kinase domain, ensuring that the receptor remains in an inactive state, while others might block the interaction between EphA8 and its ephrin ligands. These interactions and blockages are central to modulating the receptor's activity. While the intrinsic specificity of these inhibitors is vital, it's equally essential for them to have suitable pharmacokinetic properties. This ensures that they can reach their target site in sufficient concentrations and remain active for an adequate duration to exert their inhibitory effect. Additionally, the stability, solubility, and potential off-target effects of these inhibitors are key factors in their overall chemical profile. As research into Eph A8 and its role in various cellular pathways continues, the understanding and development of these inhibitors will remain at the forefront of molecular biology and chemistry endeavors.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Dasatinib | 302962-49-8 | sc-358114 sc-358114A | 25 mg 1 g | $47.00 $145.00 | 51 | |
Multi-targeted tyrosine kinase inhibitor initially developed to target BCR-ABL. Apart from BCR-ABL, dasatinib is known to inhibit several other kinases, including members of the SRC family and Eph receptors. Its broad inhibitory profile can potentially target EphA8, although its specific action on EphA8 would need verification from experimental data. | ||||||
Foretinib | 849217-64-7 | sc-364492 | 5 mg | $129.00 | 6 | |
Multi-kinase inhibitor primarily known for targeting MET and VEGFR2. Given its broad spectrum of activity, it might also inhibit EphA8, although direct evidence of EphA8 inhibition would be necessary to confirm this. | ||||||
PD 173955 | 260415-63-2 | sc-507378 | 10 mg | $320.00 | ||
Compound is a potent inhibitor of the Src family of tyrosine kinases. While its primary target is not EphA8, its broad activity across tyrosine kinases might make it effective against EphA8. | ||||||
Nilotinib | 641571-10-0 | sc-202245 sc-202245A | 10 mg 25 mg | $205.00 $405.00 | 9 | |
Like dasatinib and bosutinib, nilotinib is another BCR-ABL inhibitor used for CML. Its primary targets do not include EphA8, but given the similarities among kinases, there might be potential for EphA8 inhibition, although direct evidence would be necessary. | ||||||
Vandetanib | 443913-73-3 | sc-220364 sc-220364A | 5 mg 50 mg | $167.00 $1353.00 | ||
Primarily known as an inhibitor of VEGFR, RET, and EGFR, vandetanib's role in inhibiting EphA8 would need experimental validation. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $150.00 $388.00 | 113 | |
Natural alkaloid from the bacterium Streptomyces staurosporeus and is a potent, non-selective inhibitor of protein kinases. Given its broad-spectrum kinase inhibition activity, it might inhibit EphA8, but this would require specific experimental data. | ||||||