A cell-permeable benzothiazolo compound that acts a potent, selective, and reversible inhibitor of CKIg (IC50=290nM). Exhibits much reduced potency towards CKle and CKla isoforms (IC50=1.3 and 2.5uM, respectively). Does not affect the activity of CK2 or other kinases in a 59-protein kinase panel. Shown to block CKld-dependent period protein PER1 phosphorylation and diminish its proteasomal degradation in a dose-dependent manner. Also, shown to lengthen the circadian period in U2OS cells (10h at 8uM) without significantly affecting the amplitude of Per2-dLuc and Bmal1-dLuc rhythms.
Formula:C16H13ClN2OS
Molecular Weight:316.8
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. Reconstituted product is stable for 6 months 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.