A dual CK1δ/ε inhibitor
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PF-5006739

Item No. 46620

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-(4-fluorophenyl)-1-[1-(3-isoxazolylmethyl)-4-piperidinyl]-1H-imidazol-5-yl]-2-pyrimidinamine
CAS Number
1293395-67-1
Molecular Formula
C22H22FN7O
Formula Weight
419.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/ml
SMILES
FC1=CC=C(C(N=C2)=C(C3=CC=NC(N)=N3)N2C4CCN(CC4)CC5=NOC=C5)C=C1
InChi Code
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)
InChi Key
XPWHRQHBPRSUAW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $25

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    5 mg

    $69

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    10 mg

    $125

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    25 mg

    $281

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    PF-5006739 is a dual inhibitor of casein kinase 1δ (CK1δ) and CK1ε (IC50s = 3.9 and 17 nM, respectively).1 It is selective for CK1δ/ε over a panel of 57 kinases at 1 µM but does inhibit JNK2 and misshapen-like kinase 1 (MINK1), also known as ZC3 (IC50s = 6.1 and 1.5 µM, respectively). PF-5006739 (10 mg/kg) induces circadian phase delays in mice and cynomolgus monkeys. It prevents reinstatement of fentanyl-seeking behavior in a rat model of drug relapse. PF-5006739 also improves glucose tolerance but does not affect body weight in high-fat diet-induced obese mice and ob/ob mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wager, T.T., Chandrasekaran, R.Y., Bradley, J., et al. Casein kinase 1δ/ε inhibitor PF-5006739 attenuates opioid drug-seeking behavior. ACS Chem. Neurosci. 5(12), 1253-1265 (2014).

    2. Cunningham, P.S., Ahern, S.A., Smith, L.C., et al. Targeting of the circadian clock via CK1δ/ε to improve glucose homeostasis in obesity. Sci. Rep. 6, 29983 (2016).