| S1572 |
BS-181 HCl |
BS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9. |
Selective |
CDK7, IC50: 21 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 |
CDK7/CyclinH, IC50: 10 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 |
CDK7/CyclinH, IC50: 62 nM |
| 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 |
CDK7/CyclinH, IC50: 150 nM |
| S1230 |
Flavopiridol (Alvocidib) |
Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2. |
Pan |
CDK7, IC50: 300 nM |
| S2679 |
Flavopiridol (Alvocidib) HCl |
Flavopiridol HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2. |
Pan |
CDK7, IC50: 300 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 |
CDK7/CyclinH/MAT1, IC50: 2.4 μM |
| S8058 |
P276-00 |
P276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Phase 2/3. |
Pan |
CDK7/CyclinH, IC50: 2.87 μM |