AA cell-permeable (R)-DRF053 (Cat. No.
219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC
50 = 0.09, 0.072, 0.041, 0.11, 1.10, 0.18, and 0.40 µM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK7/H, CDK9/T, and CK1δ/ε, respectively). As is the case with (R)-DRF053, (R)-CR8 inhibits CDK/CK1 more effectively than (R)-Roscovitine (Cat. Nos.
550360 &
550364), while maintaining similar selectivity profile over other types of kinases (IC
50 = 3.6, 3.6, and 12.0 µM against Dyrk1A, Erk2, and GSK-3α/β, respectively). Both (R)-CR8 & its (S)-enantiomer (Cat. No.
203882) are much more effective than (R)-Roscovitine in apoptosis induction in cell cultures.
|
Product information
|
|
Form
|
Off-white solid
|
|
Molar mass
|
431.5
|
|
Protect from Light
|
Yes
|
|
Packaged under inert gas
|
Yes
|
|
Purity
|
≥97% by HPLC
|
|
Solubility
|
DMSO or EtOH
|
|
Chemical formula
|
C24H29N7O
|
|
Store and ship information
|
|
|
|
Storage
|
+2°C to +8°C
|
|
Ship
|
Ambient Temperature Only
Standard Handling
|