1293395-67-1

1293395-67-1 structure

Name: PF 5006739
Chemical Name: 4-{4-(4-Fluorophenyl)-1-[1-(1,2-oxazol-3-ylmethyl)-4-piperidinyl]-1H-imidazol-5-yl}-2-pyrimidinamine
CAS Number: 1293395-67-1
Molecular Formula: C₂₂H₂₂FN₇O
Molecular Weight: 419.455
Catalog: Signaling Pathways Cell Cycle/DNA Damage Casein Kinase
Create Date: 2018-07-21 04:53:37
Modify Date: 2024-01-21 09:41:01
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid drug-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner[1]. PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity[2].

Name	4-{4-(4-Fluorophenyl)-1-[1-(1,2-oxazol-3-ylmethyl)-4-piperidinyl]-1H-imidazol-5-yl}-2-pyrimidinamine
Synonyms	4-{4-(4-Fluorophenyl)-1-[1-(1,2-Oxazol-3-Ylmethyl)piperidin-4-Yl]-1h-Imidazol-5-Yl}pyrimidin-2-Amine 2-Pyrimidinamine, 4-[4-(4-fluorophenyl)-1-[1-(3-isoxazolylmethyl)-4-piperidinyl]-1H-imidazol-5-yl]- 4-{4-(4-Fluorophenyl)-1-[1-(1,2-oxazol-3-ylmethyl)-4-piperidinyl]-1H-imidazol-5-yl}-2-pyrimidinamine

Description	PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid drug-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner[1]. PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity[2].
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> Casein Kinase Research Areas >> Neurological Disease Signaling Pathways >> Stem Cell/Wnt >> Casein Kinase
Target	CK1δ:3.9 nM (IC50) CK1ϵ:17.0 nM (IC50)
References	[1]. Wager TT, et al. Casein kinase 1δ/ε inhibitor PF-5006739 attenuates opioid drug-seeking behavior. ACS Chem Neurosci. 2014 Dec 17;5(12):1253-65. [2]. Cunningham PS, et al. Targeting of the circadian clock via CK1δ/ε to improve glucose homeostasis in obesity.Sci Rep. 2016 Jul 21;6:29983.