Chemi-Verse™ CDK12/CyclinK Kinase Assay Kit

Products from BPS Bioscience require a minimum order value above 400€

Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.

Background: The CDK12/CyclinK complex comprises human CDK12 (cyclin dependent kinase 12) and human cyclinK. CDK12 is ubiquitously expressed, being present at high levels in the reproductive tissues, endocrine tissues, bone marrow and lymph nodes, predominantly in the nucleus of cells. CDK12 is involved in gene expression, transcription elongation and genome stability. CDK12 binds only to cyclinK, and the formation of this complex seems important to maintain cyclinK stability. This complex regulates phosphorylation of serine 2 in the C-terminal domain of RNA polymerase II, which is responsible for transcriptional elongation and synthesis of full-length mature mRNAs. However, lack of CDK12 seems to only affect about 5% or less of the total transcription, indicating a selective role of this complex in the transcription of certain genes. The use of inhibitors, such as THZ531, indicated that the genes being selectively regulated by CDK12/cyclinK are the core DDR (DNA damage and repair) genes. CDK12 plays a role in cancer development such as in breast and prostate cancer. The use of CDK12/cyclinK inhibitors in combination with PARP (poly-(ADP-ribose) protein) inhibitors can increase the response of cells to PARP inhibition and cell death in cases of drug resistance. The development of CDK12 inhibitors, to be used alone or in combination therapy, is a promising field of research in cancer therapy.

Contraindications: The final concentration of DMSO in the assay should not exceed 1%.

Description: The Chemi-Verse™ CDK12/CyclinK Kinase Assay Kit is designed to measure CDK12 (cyclin-dependent kinase 12)/CyclinK 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 CDK12 (amino acids 696-1082)/CyclinK complex,  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: CDK12: Q9NYV4; Cyclin K: O75909

Warnings: Avoid freeze/thaw cycles

Biosafety Level: Not applicable (BSL-1)

References: Zhang T., et al., 2016 Nat Chem Biol 12, 876 - 884.
Bösken C.A., et al., 2014 Nat Commun. 5:3505.
Choi S., et al., 2020 Experimental & Molecular Medicine 52:762-771.

• Artikelnummer: BPS82295
• Hersteller: BPS Bioscience
• Hersteller Artikelnummer: 82295
• Verpackungseinheit: 96 reactions
• Mengeneinheit: PAK