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    GSK2656157
    GSK2656157

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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 #: V0060
    CAS #: 1337532-29-2Purity ≥98%

    Description: GSK2656157 (GSK-2656157) is a novel, potent, ATP-competitive and highly selective inhibitor of PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) enzyme with IC50 of 0.9 nM in cell-free assays, it has 500-fold greater activity against a panel of 300 kinases. Treatment of GSK2656157 causes an inhibition of PERK and decreases in the downstream substrates, including phospho-eIF2α, ATF4 and CHOP. The inhibition of PERK results in effects on de novo protein synthesis as shown in BxPC3 cells.

    References: Cancer Res. 2013 Mar 15;73(6):1993-2002.

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    Molecular Weight (MW)416.45
    FormulaC23H21FN6O
    CAS No.1337532-29-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 32 mg/mL (76.83 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: <1 mg/mL
    SynonymGSK2656157; GSK 2656157; GSK-2656157
    Chemical Name1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethanone


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    In Vitro

    Kinase Assay: Inhibitory potency of GSK2656157 is measured using recombinant GST-PERK (536–1116 amino acids) with 6-His-full-length human eIF2a as a substrate. Kinase selectivity is evaluated using 27 kinases at GSK as well as a panel of 300 kinases.


    Cell Assay: human tumor cell lines, primary human microvascular endothelial cells; ~3 μM; 3 days; Antiproliferative activity of GSK2656157 against multiple human tumor cell lines as well as primary human microvascular endothelial cells is evaluated in a 3-day proliferation assay using standard culture medium. In the absence of exogeneous UPR inducers, GSK2656157 has no significant effect on the growth of any of these cells with IC50 range of 6–25 mM.

    Pretreatment of cells with GSK2656157 results in inhibition of PERK activation as well as decreases in the downstream substrates, phospho-eIF2a, ATF4, and CHOP with an IC50 in the range of 10-30 nM. Cells that are exposed to 1 mM GSK2656157 before UPR induction are able to block this effect on de novo protein synthesis. Five of 84 UPR-related genes (DDIT3, HERPUD1, PPP1R15A, C/EBP-beta, and ERN1) are down regulated more than 4-fold by GSK2656157. In the absence of exogeneous UPR inducers, GSK2656157 has no significant effect on the growth of any of these cells with IC50 range of 6–25 mM. Thus, GSK2656157 can be used to evaluate the biologic function of PERK in various biologic contexts.

    In VivoComplete inhibition of phospho-PERK Thr980 is observed through 8 hours after a single 50 mg/kg oral dose of GSK2656157. Treatment of mice with 50 or 150 mg/kg twice daily dosing of GSK2656157 results in dose-dependent inhibition of tumor growth in four models; reaching 54–114% tumor growth inhibition at the 150 mg/kg, twice daily dose. Altered amino acid metabolism, decreased blood vessel density, and vascular perfusion are potential mechanisms for the observed antitumor effect. Treatment of mice with GSK2656157 results in inhibition of tumor growth in multiple human tumor xenografts.
    Animal modelhuman tumor xenograft models
    Formulation & Dosage 00.5% hydroxypropyl methyl cellulose, 0.1% tween-80 in water (pH 6.75); 150 mg/kg; BID; Oral
    References[1] Atkins C, et al. Cancer Res, 2013, 73(6), 1993-2002.


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

     

    GSK2656157

    Cellular effect of GSK2656157 on PERK signaling and protein translation. Cancer Res, 2013, 73(6), 1993-2002.
     

    GSK2656157

     

    GSK2656157

    Vascular effects of GSK2656157 in tumor xenografts. Cancer Res, 2013, 73(6), 1993-2002.


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