GSK2656157

Catalog No.S7033

GSK2656157 Chemical Structure

Molecular Weight(MW): 416.45

GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases.

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2 Customer Reviews

  • GSK2656157 inhibits excessive autophagy in kri1lcas002 HSPCs. Representative confocal images of mCherry-Lc3 puncta (autophagosomes) in kri1lcas002 mutant embryos in Tg (cmyb: egfp) transgenic background are shown. Scale bars, 5 μm.

    Cell Res, 2015, 25: 946-962. GSK2656157 purchased from Selleck.

    The caspase-3 activation in cerebral cortex of developing brain when treatment with PERK kinase inhibitor GSK2656157 (GSK) at different dosages. a Representative immunoblots for the expression levels of cleaved caspase-3 following neonatal mice given a dose of 50, 100, and 200 mg/kg, respectively, GSK2656157 twice a day via an intragastric lavage method at P6, while the control group received same volume of vehicle. b Quantification of cleaved caspase-3 normalized to b-actin (n = 5/group). 200 mg/kg but not 50 or 100 mg/kg GSK2656157 significantly increased caspase-3 activation. Cleaved caspase-3: F = 86.69, P = 0.001 versus control. One-way ANOVA followed by post hoc test, ***P = 0.001 versus control.

    Neurotox Res, 2017, 31(2):218-229.. GSK2656157 purchased from Selleck.

Purity & Quality Control

Choose Selective PERK Inhibitors

Biological Activity

Description GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases.
Features Orally bioavailable PERK-selective inhibitor that functions independent of eIF2α phosphorylation.
Targets
PERK [1]
(Cell-free assay)
0.9 nM
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A549 cells Ml23SpVv[3Srb36gZZN{[Xl? NYfCdGNNOSCq NVv4OYh6UW6qaXLpeIlwdiCxZjD0bIFxe2mpYYLnbY4ucW6mdXPl[EBifXSxcHjvd5Bpd3K7bHH0bY9vKG:oIGDFVmshcW5iaIXtZY4hSTV2OTDj[YxteyCycnXpcoN2[mG2ZXSg[o9zKDFiaIKg[o9tdG:5ZXSgZpkhfGijcIPp[4Fz\2mwLXnu[JVkfGmxbjDt[YF{fXKnZDDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZMtKEmFNUC9NE4xOyEQvF2= NHS2fG4zPDlyMEW5Ny=>

... Click to View More Cell Line Experimental Data

In vivo Complete 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. [1]

Protocol

Kinase Assay:

[1]

+ Expand

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 Research:

[1]

+ Expand
  • Cell lines: human tumor cell lines, primary human microvascular endothelial cells
  • Concentrations: ~3 μM
  • Incubation Time: 3 day
  • Method:

    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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: human tumor xenograft models
  • Formulation: 0.5% hydroxypropyl methyl cellulose, 0.1% tween-80 in water (pH 6.75).
  • Dosages: 50 or 150 mg/kg, twice daily
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 32 mg/mL (76.83 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
1% CMC Na
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 416.45
Formula

C23H21FN6O

CAS No. 1337532-29-2
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID