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    GSK2606414
    GSK2606414

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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 #: V0059
    CAS #: 1337531-36-8Purity ≥98%

    Description: GSK2606414 is a potent and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) is also known as EIF2AK3 (Eukaryotic translation initiation factor 2-alpha kinase 3). PERK is encoded by EIF2AK3 gene. It belongs to  type I membrane protein family. It located in the ER (endoplasmic reticulum) and is induced by ER stress which is caused from malfolded proteins. 

    References: J Med Chem. 2012 Aug 23;55(16):7193-207; J Biol Chem. 1999 Feb 26;274(9):5723-30.


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    Molecular Weight (MW)451.44
    FormulaC24H20F3N5O
    CAS No.1337531-36-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 90 mg/mL (199.36 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: 19 mg/mL (42.08 mM)
    Synonym GSK2606414; GSK-2606414; GSK 2606414; GSK PERK Inhibitor.
    Chemical Name7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyrimidin-4-amine


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    In Vitro

    Kinase Assay: GST-PERK cytoplasmic domain is purchased. 6-His-full-length human eIF2α is purified from baculovirus expression in Sf9 insect cells. The eIF2α protein is buffer exchanged by dialysis into PBS, chemically modified by NHS-LC-biotin and then buffer exchanged by dialysis into 50 mM Tris, pH 7.2, 250 mM NaCl, 5 mM DTT. Protein is aliquoted and stored at −80 °C. Quench solution is freshly prepared and when added to the reaction gives final concentrations of 4 nM eIF2α phospho-ser51-antibody, 4 nM Eu-1024 labeled anti-rabbit IgG, 40 nM streptavidin Surelight APC, and 15 mM EDTA. Reactions were performed in black 384-well polystyrene low volume plates in a final volume of 10 μL. The reaction volume contains, in final concentrations, 10 mM HEPES, 5 mM MgCl2, 5 μM ATP, 1 mM DTT, 2 mM CHAPS, 40 nM biotinylated 6-His-eIF2α, and 0.4 nM GST-PERK. Compounds under analysis are dissolved in DMSO to 1.0 mM and serially diluted 1–3 with DMSO through 11 dilutions. An amount of 0.1 μL of each concentration is transferred to the corresponding well of an assay plate. This creates a final compound concentration range from 0.00017 to 10 μM. GST-PERK solution is added to assay plates containing compounds and preincubated for 30 min at room temperature. The reaction is initiated by the addition of ATP and eIF2α substrate solution. After 1 h of incubation, the quench solution is added. The plates are covered for 2 h at room temperature prior to determination of signal. The resulting signal is quantified on a Viewlux reader. The APC signal is normalized to the europium signal by transforming the data through an APC/Eu calculation. The data for concentration response curves are plotted as % inhibition calculated with the data reduction formula 100 × [1 – (U1 – C2)/(C1 – C2)] versus concentration of compound where U is the unknown value, C1 is the average control value obtained for 1% DMSO, and C2 is the average control value obtained for 0.1 M EDTA. Data are fitted with a curve described by where A is the minimum response, B is the maximum response, D is the slope factor, x is the concentration of the compound, and C is the IC50. The results for each compound are recorded as IC50 values.


    Cell Assay: In A459 cells, GSK2606414 inhibited PERK Autophosphorylation with the IC50 value of < 0.3 μM.

    In VivoGSK2606414 exhibits high oral availability, and low to moderate blood clearance in mouse, rat, and dog. GSK2606414, administered orally, inhibits tumor growth in a dose-dependent manner in mice bearing pancreatic human BxPC3 tumors.
    Animal modelBxPC3 human pancreatic xenograft model
    Formulation & Dosage 0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in water; 150 mg/kg; Oral
    References[1] Axten JM, et al. J Med Chem. 2012, 55(16), 7193-7207.


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

    GSK2606414


    PK4 inhibitor GSK2606414 prevents recrudescence following ART treatment. Cell Host Microbe. 2017 Dec 13;22(6):766-776.e4.

     

    GSK2606414

    Phosphorylation of PfeIF2α in a PfK13 C580Y mutant parasite. Cell Host Microbe. 2017 Dec 13;22(6):766-776.e4.



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