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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: SIK (salt-inducible kinases) are serine/threonine kinases of the AMPK (AMP-activated protein kinase) family. They are involved in gluconeogenesis and lipid metabolism inhibition. Dysfunction of SIK has been linked to cancer, due to its association with the TGFβ (transforming growth factor β)-Smad, AKT (protein kinase B), Hippo and NF-κB (nuclear factor kappa-light chain enhancer of activated B cells) pathways. The role of SIK proteins in cancer is complex, with some family members acting as oncogenes while others functioning as suppressors. SIK1 is present at high levels in the adrenal cortex, adipose and neural tissues. SIK1 acts as tumor suppressor in ovarian, lung, colorectal and breast cancer, pancreatic and hepatocellular carcinoma. It inhibits the epithelial-mesenchymal transition (EMT) by downregulating transcription factors involved in inhibition of E-cadherin expression, such as ZEB1 (zinc-finger E-box binding homeobox 1) and ZEB2. MicroRNAs, such as miR-141 and miR17, target SIK1 and promote cancer progression. The development of SIK inhibitors is the focus of intense research, but further studies are needed to identify isoform-specific inhibitors that can be used in cancer therapy.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ SIK1 Kinase Assay Kit is designed to measure SIK1 (salt-inducible kinase 1) 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 SIK1 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: P57059
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Sun Z., et al., 2020, Signal Transduction and Targeted Therapy 5:150.
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