PF-5006739

Product NamePF-5006739
CAS1293395-67-1
MFC22H22FN7O
MW419.45
EINECS
MOL File1293395-67-1.mol

Chemical Properties

storage temp.	room temp
solubility	Soluble in DMSO
form	powder
color	white to beige
SMILES	FC(C=C1)=CC=C1C2=C(C3=CC=NC(N)=N3)N(C4CCN(CC5=NOC=C5)CC4)C=N2

Safety Information

RIDADR	UN 2811 6.1 / PGIII
WGK Germany	WGK 3
Storage Class	6.1D - Non-combustible acute toxic Cat.3 toxic hazardous materials or hazardous materials causing chronic effects
Hazard Classifications	Acute Tox. 3 Oral

Usage And Synthesis

Uses

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].

Biochem/physiol Actions

PF-5006739 is a potent inhibitor of casein kinases 1 delta (CK1δ) and 1 epsilon (CK1ε), key regulators of the suprachiasmatic nucleus (SCN) central clock and also linked to the development of drug addiction through PERIOD proteins (PER1–3) and dopamine- and cAMP-regulated neuronal phosphoprotein (DARPP-32) modulation. PF-5006739 has low nM in vitro potency for CK1δ/ε (IC50 values of 3.9 nM for CK1δ and 17.0 nM for CK1ε) and high kinome selectivity. PF-5006739 induced profound phase delays in circadian periodicity in both nocturnal and diurnal animal models and attenuated opioid drug-seeking behavior in a rodent operant reinstatement model.

IC 50

CK1δ: 3.9 nM (IC₅₀)

storage

Store at +4°C

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. DOI:10.1021/cn500201x
[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. DOI:10.1038/srep29983

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