Table 1. In vitro biochemical activity of G1T38.
CDK4/Cyclin D1 | CDK6/Cyclin D3 | CDK9/Cyclin T | CDK5/p35 | CDK5/p25 | CDK2/Cyclin A | CDK1/Cyclin B1 | CDK7/Cyclin H/ Mat1 | CDK2/Cyclin E | |
---|---|---|---|---|---|---|---|---|---|
Mean (μM) | .001 | .002 | .028 | 0.832 | 1.2 | 1.5 | 2.4 | 2.4 | 3.6 |
Biochemical profiling of G1T38 in Nanosyn, Inc. (Santa Clara, CA) kinase screen for CDKs. The assays were completed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose response format in singlicate at Km for ATP. Results are displayed as micromolar concentrations for IC50 curves against putative target.