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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: CDK1 (cyclin-dependent kinase 1), also known as cell division cycle protein 2 homolog, belongs to the serine/threonine protein kinase family and is involved in cell cycle regulation. CDK1 is regulated by multiple partners, being activated by other CDK family members like CDK7 and CDK2, but also by CDC25C, DNMT3A (DNA (cytosine-5)-methyltransferase 3A, HDAC3 (histone deacetylase 3), myc and others. Proteins like p21, HDAC4 and SUMO1 (small ubiquitin-related modifier 1) are involved in its inactivation. CDK1 complexed with cyclins in turn regulates multiple targets, both tumor suppressors and promoters, via phosphorylation. These include HIF1α (hypoxia-inducible factor 1-alpha), BCL2 (B-cell lymphoma 2) and EZH2 (enhancer of zeste homolog 2). CDK1 is linked to several cancer types, including colon carcinoma, hepatocellular carcinoma, lung and prostate cancer. The use of inhibitors targeting CDK1 can effectively stop cancer cell proliferation and has shown great promise in preclinical studies. One example is Dinaciclib, a high affinity inhibitor of CDK1, 2, 5 and 9, for the treatment of refractory chronic lymphocytic leukemia (CLL). The use of CDK inhibitors carries side effects due to role of CDK proteins in cell biology, so the development of CDK1 specific inhibitors and a better understanding of the impact of such therapies will benefit oncology patients.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ CDK1/CyclinA2 Kinase Assay Kit is designed to measure CDK1 (cyclin dependent kinase 1)/CyclinA2 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 CDK1/CyclinA2 complex, 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: CDK1: P06493; CyclinA2: P20248
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Wang Q., et al., 2023 npj Precision Oncology 7:58
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