85-2071-93 Casein Kinase I Inhibitor III, PF-4800567 (CKI Inhibitor III, PF-4800567)(3-(3-Chlorophenoxymethyl)-1-(tetrahydropyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine, HCl) 5mg 217250
85-2071-93 Casein Kinase I Inhibitor III, PF-4800567 (CKI Inhibitor III, PF-4800567)(3-(3-Chlorophenoxymethyl)-1-(tetrahydropyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine, HCl) 5mg 217250
A cell-permeable pyrazolopyrimidinylamino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKle with ~22-fold greater potency over CKld (IC50=32 and 711nM, respectively) and displays excellent selectivity among 50-kinases, with the only exception of EGFR (69% inhibition at 1uM). Shown to preferentially block PER3 (PERIOD3) nuclear translocation in COS7-GFP-PER3-CKle cells over CKld-transfected cells (IC50=0.13 and 2.65uM, respectively), and PER2 degradation in COS7-GFP-PER2-CKle cells. Unlike Casein Kinase I Inhibitor II, PF-670462, PF-4800567 exerts only marginal effect on circadian clock under similar conditions.
Formula:C₁₇H₁₈ClN₅O₂
Molecular Weight:359.8
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.