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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: VRK1 (vaccinia-related kinase), is a member of the serine/threonine kinase family. It is found predominantly in dividing tissues, such as testis and thymus. It is a nuclear protein involved in gene regulation, DNA damage response, and cell proliferation through phosphorylation of p53, histones, and other transcription factors. Its roles in cell proliferation and DNA repair make it relevant for cancer survival and progression, and high levels of VRK1 have been found in breast, colon, lung cancer and gliomas. A reduction in VRK1 activity can thus provide benefits, and the combined use of VRK1 inhibitors and PARP inhibitors, such as an Olaparib, has been shown to contribute to synthetic lethality. The use of VRK1 inhibitors, alone or in combination therapy, may prove highly beneficial in cancer therapy.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ VRK1 Kinase Assay Kit is designed to measure VRK1 (vaccinia-related kinase) 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 VRK1 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: Q99986
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Campillo-Marcos I. and Lazo P., 2019 J Exp Clin Cancer Res 38:203.
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