Table 1.
CDK9 degradation occurs at concentrations where CDK9 target engagement is undetectable.
| Wildtype MOLT4 Cells | CRBN−/− MOLT4 Cells | ||||||
|---|---|---|---|---|---|---|---|
|
| |||||||
| Kinase | Labeling Site | SNS-032 0.25μM |
THAL-SNS-032 0.25μM |
NVP-2 0.25μM |
SNS-032 0.25μM |
THAL-SNS-032 0.25μM |
NVP-2 0.25μM |
|
| |||||||
| CDK9 | Lys2 | 34.1 | 85 | 56.9 | 15.9 | 30.7 | 63 |
| CDK6 | Lys2 | 65.3 | 11.1 | −10 | 73.8 | 6.6 | −8.6 |
| PCTAIRE1,PCTAIRE3 | Lys2 | 54.2 | 16.3 | −30.5 | 66.3 | 11.4 | −5.2 |
| PCTAIRE2 | Lys2 | 70.9 | 18.7 | 8.1 | 76.4 | 23.7 | 10.3 |
| PCTAIRE2,PCTAIRE3 | Lys1 | 70.4 | 22.1 | −4.7 | 75.4 | 16 | −15 |
| GSK3A | Lys2 | 31.6 | 41.3 | 5.8 | 40.2 | 33.8 | 10 |
Top targets of SNS-032, THAL-SNS-032, and NVP-2 in wildtype and CRBN−/− MOLT4 cells as percent inhibited. Full datasets in Supplementary Datasets 4 and 5.