A cell-permeable purine compound that acts as a reversible and ATP-competitive dual inhibitor of CKIa and CKId activities (IC50 = 5.6 and 8.8uM) with moderate selectivity over Cdk7 and Erk2 (IC50 = 29 and 52uM). Shown to block CKIa/d-mediated phosphorylation of PER1, a clock protein, (IC50 ~9uM) and repress PER1 proteasomal degradation, and lengthen the circadian period in U2OS cells (by ~13hrs at 10uM) much more effectively than Casein Kinase I Inhibitor, D4476 and IC261 and in larval zebra fish.
Formula:C16H16F3N5
Molecular Weight:335.3
Solubility:DMSO (50mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
