CDK1/CycE2 Kinase TR-FRET Detection Kit
Item | Cat# | Price |
TR-FRET Detection Kit | SNB-B-0004 | Inquiry |
Compound Test Services | CT-001 | $1,050 per 384w plate (Up To 16 cpds Dose) |
Product Description
Cyclin-dependent kinases (CDKs) are a family of serine/threonine kinases that play central roles in regulating the eukaryotic cell cycle. Their activity depends on association with specific cyclins, which control CDK activation at distinct cell cycle phases. For example, CDK4/6–cyclin D complexes drive G1 phase progression, while CDK1–cyclin B controls entry into mitosis. CDKs function by phosphorylating key substrates that govern DNA replication, mitotic entry, and transcriptional regulation. Beyond cell cycle control, several CDKs (e.g., CDK7, CDK9) are involved in transcriptional regulation via phosphorylation of RNA polymerase II. Dysregulation of CDK activity is frequently observed in cancer, leading to uncontrolled proliferation. Consequently, selective CDK inhibitors such as palbociclib, ribociclib, and abemaciclib have been developed as targeted therapies, particularly for breast cancer, underscoring the critical role of CDKs in both normal cellular homeostasis and oncogenesis.
Screeningbio’s TR-FRET CDKs kinase assay kit is designed to measure the relative activity levels of kinases. The kit uses a specific CDKs kinase substrate and detection reagents to evaluate kinase activity. Cyclin-dependent kinases (CDKs) constitute a large family, including CDK1/3/4/6/7/9/10/12/13/15–18, which specifically recognize and phosphorylate the Retinoblastoma-associated protein (Rb) at serine residue 780 (S780). Therefore, this kit employs an optimized Rb (S780) peptide as a substrate, coupled with TR-FRET LA(TR-FRET Acceptor) and TR-FRET Solar Eu conjugates(TR-FRET Donor), together with a phospho-Rb (S780)–specific antibody. This allows kinase activity to be quantified by detecting the level of phosphorylated substrate.
Data
Target Background
Cyclin-dependent kinase 1 (CDK1), also known as cell division control protein 2 homolog (CDC2), is a highly conserved serine/threonine kinase that serves as the master regulator of cell-cycle progression in eukaryotic cells. CDK1 forms active complexes with mitotic cyclins, primarily Cyclin A and Cyclin B, to drive the transition from G2 phase into mitosis (M phase). Activation of CDK1 requires binding to its cyclin partner and precise phosphorylation–dephosphorylation events, particularly activating phosphorylation at threonine 161 and removal of inhibitory phosphates at threonine 14 and tyrosine 15 by the Cdc25 phosphatase.
Once activated, the CDK1/cyclin complex phosphorylates numerous substrates involved in chromatin condensation, nuclear envelope breakdown, spindle assembly, and cytokinesis, thereby ensuring accurate chromosome segregation and cell division. CDK1 activity is tightly regulated by checkpoint pathways that monitor DNA integrity and replication status, preventing premature mitotic entry.
Because CDK1 is essential for cell proliferation, its dysregulation can lead to genomic instability and uncontrolled cell growth, contributing to oncogenesis. Conversely, excessive inhibition of CDK1 can cause mitotic arrest and apoptosis. Owing to its central role in cell-cycle control, CDK1 has become a major therapeutic target for anticancer drug development aimed at selectively disrupting mitotic progression in tumor cells.