2. Cell Cycle/DNA Damage
    Stem Cell/Wnt
  3. Casein Kinase
  4. PF-670462 dihydrochloride

PF-670462 dihydrochloride 

Cat. No.: HY-15490 Purity: 99.96%
COA Handling Instructions

PF-670462 dihydrochloride is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.

For research use only. We do not sell to patients.

PF-670462 dihydrochloride Chemical Structure

PF-670462 dihydrochloride Chemical Structure

CAS No. : 950912-80-8

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Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 145 In-stock
Solid
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50 mg USD 495 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PF-670462 dihydrochloride purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2020 Mar 12;523(3):809-815.  [Abstract]

    Immunoblot analysis of cells treated with IC261 or PF670462 for 48 h. GAPDH served as a loading control.

    PF-670462 dihydrochloride purchased from MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531.   [Abstract]

    CK1ε phosphorylates LRP6 at Thr1479 in vitro and TPA enhances the kinase activity of CK1ε. GST-LRP6 mini fragment fusion protein is incubated with recombinant CK1ε in the presence of 200 μM ATP with or without 160 μM TPA or 2 μM PF670462 as indicated.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PF-670462 dihydrochloride is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.

    IC50 & Target[1]

    CKIδ

    14 nM (IC50)

    EGFR

    150 nM (IC50)

    SAPK2A/p38

    190 nM (IC50)

    In Vitro

    PF-670462 is a potent and selective inhibitor of CKIε and CKIδ, with IC50s of 7.7 nM and 14 nM, respectively. PF-670462 shows less than 30-fold selevtivity for EGFR and SAPK2A/p38, with IC50s of 150 nM and 190 nM, respectively. PF-670462 also causes a redistribution of the GFP signal to the cytoplasm in a concentration-dependent manner, with an EC50 of 290 ± 39 nM in CKIε-transfected COS7 cells[1]. PF-670462 is a potent inhibitor of Wnt/β-catenin signaling, with an IC50 of ∼17 nM. PF-670462 (1 μM) is a weak inhibitor of proliferation, and only modestly suppresses the growth of HEK293 and HT1080 cells. PF-670462 (100 nM) strongly inhibits CK1ε and CK1δ, consistent with its effect on Wnt/β-catenin signaling[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    PF-670462 (50 mg/kg, s.c.) produces robust phase delays, and the activity remains persistent, with no discernible correction in the absence of exogenous zeitgebers in rats. PF-670462 (25, 50, and 100 mg/kg, s.c.) induces dose-dependent phase shift[1]. PF-670462 (50 mg/kg; s.c.) significantly phase delays the rhythmic transcription of Bmal1, Per1, Per2 and Nr1d1 in both liver and pancreas by 4.5 ± 1.3 h and 4.5 ± 1.2 h, respectively, 1 day after administration. In the suprachiasmatic nucleus (SCN), the rhythm of Nr1d1 and Dbp mRNA expression is also delayed by 4.2 and 4 h, respectively[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    410.32

    Appearance

    Solid

    Formula

    C19H22Cl2FN5
    CAS No.
    SMILES

    NC1=NC=CC(C2=C(C3=CC=C(F)C=C3)N=CN2C4CCCCC4)=N1.[H]Cl.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (243.71 mM; Need ultrasonic)

    DMSO : ≥ 32 mg/mL (77.99 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4371 mL 12.1856 mL 24.3712 mL
    5 mM 0.4874 mL 2.4371 mL 4.8742 mL
    10 mM 0.2437 mL 1.2186 mL 2.4371 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  PBS

      Solubility: 25 mg/mL (60.93 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (5.07 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (5.07 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.96%

    COA (259 KB) HNMR (207 KB) LCMS (119 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    The CKIε kinase assay is performed in a 40-μL final volume in buffer containing 50 mM Tris, pH 7.5, 10 mM MgCl2, 5 mM dithiothreitol with 5 μM ATP, 3 nM CKIεΔ319, and 15 μM peptide substrate PLSRTLpSVASLPGL in the presence of 5 μL of CKIε inhibitor (PF-670462) or 5% dimethyl sulfoxide. The reaction is incubated for 3 h at 27°C; detection is carried out as described for the Kinase-Glo Assay. Luminescent output is measured[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Adult male CD rats (initial weight 175-225 g) are released into constant darkness (DD) for 2 weeks, and their individual free-running periods and times of activity onset are determined from the 7 to 10 days at the end of the 2-week period. Dosing of 50 mg/kg PF-670462 or vehicle (40% β-cyclodextrin) takes place at circadian time (CT)9 or 3 h before the predicted onset of activity; night vision goggles facilitated the subcutaneous administration. CT9 is chosen based on preliminary data demonstrating robust responses to CKIε inhibition at this circadian time. Animals are maintained under DD for an additional 4 to 5 days postdose, and the data from that time period are used in the estimation of the magnitude and direction of the putative phase shifts[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    PF-670462950912-80-8PF670462PF 670462Casein KinaseInhibitorinhibitorinhibit

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