| S2768 |
Dinaciclib (SCH727965) |
Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM, respectively. It also blocks thymidine (dThd) DNA incorporation. Phase 3. |
Pan |
CDK5, IC50: 1 nM |
| S1487 |
PHA-793887 |
PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. Phase 1. |
Pan |
CDK5/p25, IC50: 5 nM |
| S1524 |
AT7519 |
AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. Phase 2. |
Pan |
CDK5/p35, IC50: 13 nM |
| S1153 |
Roscovitine (Seliciclib,CYC202) |
Roscovitine (Seliciclib, CYC202) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM. It shows little effect on CDK4/6. Phase 2. |
Pan |
CDK5/p35, IC50: 0.16 μM |
| S2751 |
Milciclib (PHA-848125) |
Milciclib (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2. |
Pan |
CDK5/p35, IC50: 265 nM |
| S1145 |
SNS-032 (BMS-387032) |
SNS-032 has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. Phase 1. |
Pan |
CDK5/p35, IC50: 340 nM |
| S2742 |
PHA-767491 |
PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.It displays ~20-fold selectivity against CDK1/2 and GSK3-β, 50-fold selectivity against MK2 and CDK5, 100-fold selectivity against PLK1 and CHK2. |
Pan |
CDK5, IC50: 460 nM |