CDK2 Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
|Selective||CDK2, Ki: 46 nM|
|S2735||MK-8776 (SCH 900776)||
SCH 900776 is a selective Chk1 inhibitor with IC50 of 3 nM. It shows 500-fold selectivity against Chk2. Phase 2.
|Selective||CDK2, IC50: 0.16 μM|
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||CDK2, IC50: 1 nM|
JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
|Pan||CDK2/CyclinE, IC50: 3 nM; CDK2/CyclinA, IC50: 4 nM|
R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.
|Pan||CDK2/CyclinE, Ki: 3 nM|
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||CDK2, IC50: 6 nM|
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||CDK2/CyclinE, IC50: 8 nM; CDK2/CyclinA, IC50: 8 nM|
BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM. It is 25-fold more selective for CDK1/2 than CDK4.
|Pan||CDK2/CyclinE, IC50: 9 nM|
SU 9516 is a 3-substituted indolinone CDK inhibitor with IC50 of 22 nM, 40 nM, and 200 nM for CDK2, CDK1, and CDK4, respectively.
|Pan||CDK2, IC50: 22 nM|
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||CDK2/CyclinE, IC50: 48 nM; CDK2/CyclinA, IC50: 38 nM|
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||CDK2, IC50: 40 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||CDK2, IC50: 40 nM|
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||CDK2/CyclinE, IC50: 363 nM; CDK2/CyclinA, IC50: 45 nM|
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||CDK2/CyclinA, IC50: 47 nM|
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||CDK2/CyclinA, IC50: 224 nM; CDK2/CyclinE, IC50: 2.54 μM|
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||CDK2, IC50: 240 nM|
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||CDK2/CyclinE, IC50: 0.7 μM; CDK2/CyclinA, IC50: 0.7 μM|
NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.
|Pan||CDK2, Ki: 1.3 μM|
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.
|Pan||CDK2, IC50: 2.441 μM|