1188296-52-7

PF-4800567 is a selective inhibitor of casein kinase 1ε (CK1ε; IC₅₀ = 32 nM) with greater than 20-fold selectivity over CK1δ. It blocks CK1ε-mediated PER3 nuclear localization and PER2 degradation, both of which are proteins important for maintaining circadian rhythms in cells. PF-4800567 has been used in the study of the CK1 enzymes in the regulation of circadian rhythm and is also reported to have neuroprotective effects.

PF 4800567 is a selective casein kinase 1ε inhibitor; displays 22-fold greater potency towards CK1ε than CK1δ (IC50 values are 32 and 711 nM for CK1ε and CK1δ respectively). ATP competitive. Displays minimal effect on the circadian clock.

ChEBI: PF-4800567 is a pyrazolopyrimidine that is 1H-pyrazolo[3,4-d]pyrimidin-4-amine which is substituted at positions 1 and 3 by tetrahydro-2H-pyran-4-yl and (m-chlorophenoxy)methyl groups, respectively. It is a selective inhibitor of the epsilon isoform of casein kinase 1 (CK1epsilon). It has a role as an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor. It is a pyrazolopyrimidine, a member of monochlorobenzenes, an aromatic ether and a member of oxanes.

CKIδ: 711 nM (IC₅₀)

Store at -20°C

[1] KEVIN M WALTON. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period.[J]. Journal of Pharmacology and Experimental Therapeutics, 2009, 330 2: 430-439. DOI: 10.1124/jpet.109.151415
[2] QING-JUN MENG. Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2010: 15240-15245. DOI: 10.1073/pnas.1005101107
[3] DANIEL I. PEREZ  Ana M  Carmen Gil. Protein kinases CK1 and CK2 as new targets for neurodegenerative diseases[J]. Medicinal Research Reviews, 2011, 31 6: 924-954. DOI: 10.1002/med.20207