PF-5006739

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 agent-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].

Product Specifications

CAS Number

[1293395-67-1]

UNSPSC

12352005

Hazard Statement

H301

Target

Casein Kinase

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Stem Cell/Wnt

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/pf-5006739.html

Purity

99.94

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

NC1=NC=CC(C2=C(C3=CC=C(F)C=C3)N=CN2C4CCN(CC5=NOC=C5)CC4)=N1

Molecular Formula

C22H22FN7O

Molecular Weight

419.45

Precautions

H301

References & Citations

[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.