PF-5006739

• CAT Number: I011989
• CAS Number: 1293395-67-1
• Molecular Formula: C22H22FN7O
• Molecular Weight: 419.46
• Purity: ≥95%
• Synonyms: PF-5006739; PF 5006739; PF5006739.;4-[4-(4-Fluorophenyl)-1-[1-(3-isoxazolylmethyl)-4-piperidinyl]-1H-imidazol-5-yl]-2-pyrimidinamine
• Target: Potent CK1δ/ε inhibitor
• Solubility: Soluble in DMSO
• Storage: room temp
• IUPAC Name: 4-[5-(4-fluorophenyl)-3-[1-(1,2-oxazol-3-ylmethyl)piperidin-4-yl]imidazol-4-yl]pyrimidin-2-amine
• InChI: InChI=1S/C22H22FN7O/c23-16-3-1-15(2-4-16)20-21(19-5-9-25-22(24)27-19)30(14-26-20)18-6-10-29(11-7-18)13-17-8-12-31-28-17/h1-5,8-9,12,14,18H,6-7,10-11,13H2,(H2,24,25,27)
• InChIKey: XPWHRQHBPRSUAW-UHFFFAOYSA-N
• SMILES: C1CN(CCC1N2C=NC(=C2C3=NC(=NC=C3)N)C4=CC=C(C=C4)F)CC5=NOC=C5

PF-5006739（Cat No.:I011989） is a potent inhibitor of CK1δ/ε (casein kinase 1 delta/epsilon). It has shown to attenuate opioid drug-seeking behavior and exhibits a desirable profile with low nanomolar potency for CK1δ/ε (IC50 = 3.9 and 17.0 nM, respectively). PF-5006739 demonstrates high selectivity within the kinome. In animal models, it effectively delays circadian rhythm and reduces opioid drug-seeking behavior in a dose-dependent manner.

Reference

1: Cunningham PS, Ahern SA, Smith LC, da Silva Santos CS, Wager TT, Bechtold DA. Targeting of the circadian clock via CK1δ/ε to improve glucose homeostasis in obesity. Sci Rep. 2016 Jul 21;6:29983. doi: 10.1038/srep29983. PubMed PMID: 27439882; PubMed Central PMCID: PMC4954991.2: Wager TT, Chandrasekaran RY, Bradley J, Rubitski D, Berke H, Mente S, Butler T, Doran A, Chang C, Fisher K, Knafels J, Liu S, Ohren J, Marconi M, DeMarco G, Sneed B, Walton K, Horton D, Rosado A, Mead A. Casein kinase 1δ/ε inhibitor PF-5006739 attenuates opioid drug-seeking behavior. ACS Chem Neurosci. 2014 Dec 17;5(12):1253-65. doi: 10.1021/cn500201x. Epub 2014 Oct 28. PubMed PMID: 25299732.