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: Cyclin-dependent kinase 9 (CDK9) is the catalytic subunit of the positive transcription elongation factor b (P-TEFb) complex, which phosphorylates the C-terminal domain of RNA polymerase II, a key player in the production of mature RNA. P-TEFb also includes cyclin T. CDK9 translocates to the nucleus once it gets auto phosphorylated, where it can associate with cyclin T. Hyperactivation of cyclins is known to result in cancer and the development of resistance to therapy, and CDK9-cyclin T is involved in the transcription of oncogenes. The inhibition or degradation of specific CDK-cyclin complexes could prove beneficial in cancer treatment, but the development of specific inhibitors has been difficult. Recently a small molecule degrader specific for CDK9-cyclin T was identified, LL-K9-3, which resulted in lower levels of androgen receptor (AR) and cMyc in 22RV1 cells. LL-K9-3 thus seemed more effective than SNS032, its parental CDK9 inhibitor, and the CDK9 PROTAC Thal-SNS032. Further research into new and more specific molecules will prove beneficial for cancer therapy.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ CDK9/CyclinT Kinase Assay Kit is designed to measure CDK9 (cyclin dependent kinase 9)/Cyclin T kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 384-well format, with enough purified recombinant CDK9/Cyclin T kinase, kinase substrate, ATP, and kinase assay buffer for 400 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: CDK9: P50750; CyclinT1: O60563
Warnings: Avoid freeze/thaw cycle
Biosafety Level: Not applicable (BSL-1)
References: Napolitano G, et al., 2003 J Cell Physiol. 197(1):1-7.
Li J., et al., 2022 J Med Chem. 65(16):11034-11057.