CDK9-selektive Inhibitors

  • CDK1
  • CDK2
  • CDK3
  • CDK4
  • CDK5
  • CDK6
  • CDK7
  • CDK9
  • CLK
  • Cdc
Kat.-Nr. Produktname Informationen Selektiv / Pan IC50 / Ki
S7461 LDC000067 LDC000067 is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7. Selective CDK9, IC50: 44 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 CDK9/CyclinT, IC50: 4 nM
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 CDK9, IC50: 4 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 CDK9/CyclinT, IC50: <10 nM
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 CDK9/CyclinT1, IC50: 20 nM
S2621 AZD5438 AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM. It is less potent to CDK5/6 and also inhibits GSK3β. Phase 1. Pan CDK9, IC50: 20 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 CDK9, IC50: 34 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 CDK9/CyclinT1, IC50: 138 nM