504651 PERK Inhibitor II, GSK2656157 - Calbiochem

504651
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₃H₂₁FN₆O

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      Glass bottle 5 mg
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      Description
      OverviewA cell-permeable pyrrolopyrimidinamine compound that acts as a potent, ATP-competitive EIF2AK3/PERK inhibitor (IC50 = 0.9 nM; [ATP] = 10 µM), displaying ≥511-fold selectivity over HRI/EIF2AK1, BRK, PKR/EIF2AK2, and MEKK2 (IC50 = 460, 822, 905, and 954 nM, respectively) and much reduced or little activity toward more than 300 other kinases. Potently prevents ER stress-induced enhancement of PERK and eIF2α phosphorylation as well as ATF4 & CHOP upregulation in human BxPC3 and murine LL/2 cultures in vitro (IC50 ≤30 nM; 1 h drug preincubation prior to 6 h 1 µM Thapsigargin treatment, Cat. No. 586005) and exhibits antitumor efficacy against 3 pancreas and 1 multiple myeloma xenografts in mice (54-110% tumor growth inhibition; 150 mg/kg/12 h via p.o.) in vivo. More selective than GSK2606414 (Cat. No. 516535).
      Catalogue Number504651
      Brand Family Calbiochem®
      SynonymsBRK Inhibitor II, EIF2AK1 Inhibitor II, EIF2AK2 Inhibitor III, EIF2AK3 Inhibitor II, HRI Inhibitor II, MEKK2 Inhibitor I, PKR Inhibitor III, PKR-like ER Kinase Inhibitor II
      References
      ReferencesAtkins, C., et al. 2013. Cancer Res. 73, 1993.
      Product Information
      FormWhite powder
      Hill FormulaC₂₃H₂₁FN₆O
      Chemical formulaC₂₃H₂₁FN₆O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationPERK Inhibitor II, GSK2656157, CAS 1337532-29-2 is a cell-permeable, potent, ATP-competitive inhibitor of PERK/EIF2AK3 (IC50 = 0.9 nM).
      Biological Information
      Primary TargetPERK
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Regulatory Review
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      PERK Inhibitor II, GSK2656157 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Atkins, C., et al. 2013. Cancer Res. 73, 1993.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision10-March-2014 JSW
      SynonymsBRK Inhibitor II, EIF2AK1 Inhibitor II, EIF2AK2 Inhibitor III, EIF2AK3 Inhibitor II, HRI Inhibitor II, MEKK2 Inhibitor I, PKR Inhibitor III, PKR-like ER Kinase Inhibitor II
      DescriptionA cell-permeable pyrrolopyrimidinamine compound that acts as a potent, ATP-competitive EIF2AK3/PERK inhibitor (IC50 = 0.9 nM; [ATP] = 10 µM), displaying ≥511-fold selectivity over HRI/EIF2AK1, BRK, PKR/EIF2AK2, and MEKK2 (IC50 = 460, 822, 905, and 954 nM, respectively) and much reduced or little activity toward more than 300 other kinases. While GSK2656157 potently inhibits ER stress-induced enhancement of PERK and eIF2α phosphorylation as well as ATF4 & CHOP upregulation in human PxBC3 and murine LL/2 cultures in vitro (IC50 ≤30 nM; 1 h drug preincubation prior to 6 h ER-stress induction by 1 µM Thapsigargin, Cat. No. 586005), only basal PERK phosphorylation, but not basal eIF2α phosphorylation or ATF4 & CHOP expression, is seen inhibited in pancreas (by >95% up to 8 h post single 50 mg/kg oral dose) and tumor tissues upon GSK2656157 administration in mice in vivo, resulting in the observed antitumor efficacy (54-110% tumor growth inhibition; 150 mg/kg/12 h via p.o.) and reversible pancreas damage (44% and 95% of control pancreas mass, respectively, 1 d and 15 d post 14 d 150 mg/kg/12 h oral dosing). Comparing to its structural analog GSK2606414 (Cat. No. 516535), GSK2656157 exhibits much reduced potency toward Aurora B, MLK2/MAP3K10, MLCK2/MYLK2, c-MER (IC50 = 1.259, 2.796, 3.039, and 3.431 µM, respectively), c-Kit, and DDR2 (69.84% and 25.41% inhibition, respectively, at 10 µM)
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₃H₂₁FN₆O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Regulatory Review
      ReferencesAtkins, C., et al. 2013. Cancer Res. 73, 1993.