The DIANA CDK Panel is an advanced selectivity profiling tool designed for drug discovery, enabling the precise measurement of enzyme inhibition constants (Ki) for target compounds against a comprehensive set of 24 Cyclin Dependent Kinases (CDKs). Utilizing the innovative DNA-linked Inhibitor Antibody Assay (DIANA), this ultrasensitive panel offers a wide dynamic range, ensuring reliable Ki determination from a single well in a multi-well plate format. CDKs, which are serine/threonine kinases essential for regulating the cell cycle, transcription, and pre-mRNA splicing, are critical in understanding disease mechanisms, particularly in neurodegeneration and cancer. The DIANA CDK Panel provides a robust and highly sensitive solution for researchers aiming to profile CDK inhibitors and advance their drug discovery efforts.
DIANA is a multi-well plate assay, where target protein is selectively captured to the solid carrier and then bound by a unique detection probe consisting of a small-molecule ligand linked to a DNA-oligonucleotide. Subsequently, the probe is detected and quantified by qPCR. For drug discovery, the assay utilizes competition between the probe and the test compounds to measure their binding affinity. DIANA is straightforward to develop for new targets and easy to implement using standard laboratory equipment.
DIANA Kinase Panel, which currently enables rapid potency and selectivity profiling of target compounds against approximately 150 kinases, representing clinically relevant kinases from all kinase families (AGC, CAMK, CK1, CMGC, STE, TK, TKL).
The gradual panel expansion is introducing the complete subsets corresponding to specific kinase families. As an example, the first complete DIANA CDK Panel is available for small molecules profiling
DIANA CDK Panel: 24 Cyclin Dependent Kinases (CDKs) detectable
CDK | Dynamic Range (fold change) | MIN Ki (nM; 1µM cpd used) | MAX Ki (nM; 1µM cpd used |
---|---|---|---|
CDK1/cycB1 | 15 | 110 | 1700 |
CDK2/cycA2 | 2100 | 1.0 | 2200 |
CDK3/cycE1 | 1600 | 1.4 | 2300 |
CDK4/cycD1 | 7.7 | 130 | 1000 |
CDK4/cycD2 | 13 | 130 | 1900 |
CDK4/cycD3 | 45 | 44 | 1900 |
CDK5/p25 | 550 | 3.4 | 1900 |
CDK5/p35 | 17 | 77 | 1300 |
CDK6/cycD1 | 17 | 77 | 1300 |
CDK6/cycD2 | 5.4 | 330 | 1800 |
CDK6/cycD3 | 26 | 69 | 1800 |
CDK7/cycH | 15 | 69 | 1000 |
CDK7/cycH/MNAT1 | 1500 | 0.9 | 1300 |
CDK8/cycC | 13 | 93 | 1200 |
CDK9/cycT1 | 320 | 2.8 | 900 |
CDK9/cycT2 | 290 | 3.5 | 1000 |
CDK10/cycQ | 120 | 5.4 | 650 |
CDK11A | 50 | 45 | 2300 |
CDK12/cycK | 62 | 35 | 2200 |
CDK13/cycK | 150 | 25 | 3800 |
CDK14/cycY | 330 | 5.7 | 1900 |
CDK17/cycY | 550 | 2.2 | 1200 |
CDK18/cycY | 76 | 25 | 1900 |
Bold = Transcriptional CDKs | no Bold = Cell Cycle Kinases