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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: CDC-like kinase 1 (CLK1) is part of the dual-specificity protein kinase (DSK) family that phosphorylateserine/ arginine rich (SR) proteins that are part of the spliceosomal complex and regulate non-splicing proteins. It is involved in cell cycle progression, apoptosis, the DNA replication checkpoint, and regulation of telomere length. Dysfunctions in pathways regulated by CLK1 result in Alzheimer's disease, Duchenne's muscular dystrophy (DMD), viral replication, autophagy-associated diseases (diabetes, cardiovascular, and infectious diseases) and cancer. CLK1 is upregulated in prostate cancer, gastric, and pancreatic ductal adenocarcinoma. The use of TG003, a CLK1/2/4 inhibitor, leads to dystrophin exon31 skipping in cells from DMD patients, and a partially functional dystrophin protein. TG003 also decreases gastric and prostate cancer cell viability and migration. CLK1 inhibitors such as NIH39 and KH-CB19 showed anti-viral activity towards influenza A, and Leucettine L41 increases cellular autophagy in U-2 OS cells. The development of CLK1 inhibitors and a deeper understanding of its role in the multiple pathways where it is involved will prove crucial for the treatment of CLK1-linked diseases.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ CLK1 Kinase Assay Kit is designed to measure CLK1 (CDC2-like 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 CLK1 kinase (amino acids 129-end), 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: P49759
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Song M., et al., 2023 Signal Transduction and Targeted Therapy 8: 148.