Product Name: PAK4 (471-477) pS474
Product Number: PE-04AED99
Size: | 200 µg | | Price: | 42.00 |
| 1 mg | | $US | 84.00 |
| 5 mg | | | 185.00 |
Peptide Name: PAK4 (471-477) pS474
Product Use: Services as a blocking peptide for use with the PAK4-pS474 rabbit polyclonal antibody (Cat. No.: AB-PK752) that is also available from Kinexus. This phosphopeptide may also be useful as a substrate for screening the phosphatase activity of protein phosphatases. The peptide sequence is located in the protein kinase catalytic domain activation T loop region between subdomains VII and VIII. S474 phosphorylation stimulates phosphotransferase activity.
Peptide Production Method: Solid-phase peptide synthesis
Peptide Origin: Homo sapiens
Peptide Sequence: RRK-pS-LVG
Peptide Modifications N Terminus: Free amino
Peptide Modifications C Terminus: βAla-Cys
Scientific Background: PAK4 is a protein-serine/threonine kinase of the STE group and STE20 family and PAKB subfamily. It is highly expressed and widely distributed in most tested human tissues. It stimulates cell survival, inhibits apoptosis, and also plays a role in cell cycle progression. PAK4 has been implicated in the regulation of cytoskeletal organization, and cell morphology, motility and transformation. Binding of GTP-bound Cdc42 to the autoregulatory region at the N-terminus of PAK4 releases monomers from the autoinhibited dimer, enables phosphorylation at S474 and activation of its phosphotransferase activity. It phosphorylates and inactivates the protein phosphatase SSH1, which leads to increased inhibitory phosphorylation of the actin binding/depolymerizing factor cofilin and stabilization of actin filaments. It phosphorylates LIMK1, a kinase that also inhibits the activity of cofilin. Other substrates include integrin beta5/ITGB5, ARHGEF2, RAN, and BAD. It inhibits apoptosis by preventing caspase-8 binding to death domain receptors in a kinase independent manner. It plays a role in cell-cycle progression by controlling levels of the cell-cycle regulatory protein CDKN1A. PAK4 mutations are associated with increased carcinoma cell motility and influenced inhibitor sensitivity. The protein kinase was found to be necessary for oncogenic transformation of breast cancer cells.