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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: PAK4 (p-12-activated kinase 4) is a member of the PAK family of serine/threonine kinases. The PAK family is highly evolutionary conserved and regulates cell survival, apoptosis, cytoskeleton dynamics, and other critical cellular functions. PAK4 belongs to group II, which can be activated by Cdc42 (cell division control protein 42) only as opposed to group I, which depends on either Rac1 or Cdc42.I It is ubiquitously expressed, participating in cytoskeleton remodeling, cell motility, apoptosis, and metastasis. PAK4 is regulated by HGF (hepatocyte growth factor), PKA (protein kinase A), CDK5RAP3 (CDK5 regulatory subunit associated protein 3) and SH3RF2 (SH3 domain containing ring finger 2), and in turn phosphorylates proteins like p120-catenin, SMAD2 and β-catenin. Upregulation of PAK4 has been found in multiple cancers, such as ovarian, breast and gastric cancer. Inhibition of PAK4 leads to milder cancer cell migration and invasion, and to regulation of the immune response to cancer, such as T cell infiltration. Interestingly, it was observed that the cell line HCT116, a KRAS-driven cell line, is highly sensitive to PAK4 inhibition. The development of specific inhibitors targeting PAK4, to be used alone or as combination therapy, will greatly benefit the cancer therapy field.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ PAK4 Kinase Assay Kit is designed to measure PAK4 (p21-activated kinase 4) serine/threonine kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified recombinant PAK4 kinase, kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: O96013
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Wang H., et al., 2021 Expert Opin Ther Pat. 31(11): 977-987.Li Y., et al., Front Pharmacol. 13:956220.
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