DIANA CDK Panel: Panel of 24 cyclin dependent kinases

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.

Main DIANA CDK Assay Features

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


  • ​Quantitative PCR-based readout → Ki from a single well.

  • Low consumption of reagents → cost-effective.​

  • 384-well plate format → high-throughput.​

  • Rapid inhibitor selectivity profiling against CDKs.​

  • Any CDK included in the DIANA CDK inhibitor profiling panel can be used in HTS campaigns (Z’ > 0.7) using our in-house compound libraries.

Calculation of Ki values from the concentration range of the inhibitors

Axis description:x: Ki (nM); log scale; y: Cpd concentration (nM); log scale

Ki’s comparison of the three selected inhibitors with a reference CRO measurement

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Profiling of selected kinase inhibitors by DIANA CDK panel (Kis’)

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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

Collaboration

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