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    PF-06260933 2HCl
    PF-06260933 2HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V3216
    CAS #: 1811510-56-1 (free base); 2118243-34-6 (HCl); 1883548-86-4 (2HCl)Purity ≥98%

    Description: PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 (Mitogen-activated protein kinase kinase kinase kinase 4) with IC50 values of 3.7 and 160 nM for cell-freel assay (kinase) and cell assay, respectively. It also inhibits MINK and TNIK with IC50 values of 8 and 13 nM, respectively. PF-06260933 has been reported to improve fasting hyperglycemia in mice. Recent studies in adipose tissue, pancreas, muscle, and macrophages suggest that MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic drugs. As part of the evaluation of MAP4K4 as a novel antidiabetic target, PF-6260933.

    References:  2015 Oct 6;6(11):1128-33;  2015 Dec 21;6:8995.


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    Molecular Weight (MW) 369.67
    FormulaC16H15Cl3N4 
    CAS No.1811510-56-1 (free base); 2118243-34-6 (HCl); 1883548-86-4 (2HCl)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: >50 mg/mL
    Water: 
    Ethanol: 
    Chemical Name 5-(4-Chlorophenyl)-[3,3'-bipyridine]-6,6'-diamine dihydrochloride
    Synonyms PF-06260933 2HCl; PF 06260933 2HCl; PF06260933 2HCl; PF-06260933 dihydrochloride; PF 06260933 dihydrochloride; PF06260933 dihydrochloride
    SMILES Code NC1=C(C2=CC=C(Cl)C=C2)C=C(C(C=N3)=CC=C3N)C=N1.[H]Cl.[H]Cl


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    In Vitro

    In vitro activity: PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 with IC50 values of 3.7 and 160 nM for cell-freel assay (kinase) and cell assay, respectively. It also inhibits MINK and TNIK with IC50 values of 8 and 13 nM, respectively. PF-06260933 has been reported to improve fasting hyperglycemia in mice. Recent studies in adipose tissue, pancreas, muscle, and macrophages suggest that MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic drugs. As part of the evaluation of MAP4K4 as a novel antidiabetic target, PF-6260933.


    Kinase Assay: Aortas were lysed in 1% NP-40, 50 mM Tris pH 7.4, 150 mM NaCl, 50 mM EDTA with 1 × HALT protease and phosphatase inhibitors (Thermo Scientific) and immunoprecipitated with Bethyl MAP4K4 antibodies (503 A; 1 μg) or normal rabbit IgG (Cell Signaling 2729; 1 μg). Myelin basic protein (MBP) (1 μg) and 10 μCi of [γ-32P]ATP were added to the immunoprecipitates and incubated for 30 min at 30 °C in kinase buffer (20 mM HEPES, 10 nM MgCl2, 1 mM dithiothreitol (DTT) and protease and phosphatase inhibitor cocktail). Samples were separated by 12% SDS–polyacrylamide gel electrophoresis and visualized by autoradiography.


    Cell Assay: HUVECs are maintained in EGM2 media at 37°C and 5% CO2. HUVECs or peritoneal macrophages are treated with vehicle or PF-06260933 in vitroto determine whether pharmacological inhibition of MAP4K4 alteres MAPK signalling in response to TNF-α

    In Vivo At 6–8 weeks of age, male flox/flox and flox/flox/cre+ littermates were injected with 1 mg tamoxifen per day in corn oil for 5 days. At 5–6 weeks of age (KD mice) or 2 weeks after tamoxifen injection (flox mice), the mice were fed chow or WD (0.2% cholesterol, TD 88137, Harlan Laboratories) for 16 weeks. Compound PF-06260933 (10 mg kg−1, dissolved in dH2O) was orally administered to 8–10-week-old male ApoE−/− mice twice daily for 6 weeks. Ldlr−/− male mice (B6.129S7-Ldlrtm1Her/J, Jackson Laboratories, 8–10 weeks old) were placed on HFD (1.25% cholesterol, TD96121, Harlan Laboratories) for 10 weeks before drug administration. Compound PF-06260933 was administered to male 8–10-week-old Ldlr−/− mice as above for 10 weeks. Oral administration of water was used as vehicle control in all studies. Mice were euthanized by CO2 inhalation followed by bilateral pneumothorax. No statistical methods were used to predict sample size, no randomization was performed and the investigations were not blinded during the knockout animal analyses, but were blinded during the drug treatment analyses.
    Animal model 6–8 weeks of age, male flox/flox and flox/flox/cre+ littermates
    Formulation & Dosage Dissolved in dH2O; 10 mg/kg; orally administered
    References  2015 Dec 21;6:8995;  2015 Oct 6;6(11):1128-33.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    PF-06260933 2HCl

    Pharmacological MAP4K4 inhibition ameliorates atherosclerosis.  2015 Dec 21;6:8995. 

     

    PF-06260933 2HCl

    (a) Effects of 16 (PF-06260933 ) on LPS-induced TNFα levels in C57-BL/6J mice). (b) Effects of 16 on glycemic control in ob/ob mice.  2015 Oct 6;6(11):1128-33.

     

    PF-06260933 2HCl

    Total and free plasma concentration of 16 (PF-06260933 )after PO dosing (10 mg/kg) to mice.  2015 Oct 6;6(11):1128-33.

     

    PF-06260933 2HCl

    Heat map obtained from an Invitrogen selectivity panel (% inhibition of kinases tested @1 μM).  2015 Oct 6;6(11):1128-33.

     

    PF-06260933 2HCl

     2015 Oct 6;6(11):1128-33.



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