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504651 PERK Inhibitor II, GSK2656157 - CAS 1337532-29-2 - Calbiochem

PERK Inhibitor II, GSK2656157, CAS 1337532-29-2 is a cell-permeable, potent, ATP-competitive inhibitor of PERK/EIF2AK3 (IC50 = 0.9 nM).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: EIF2AK1 Inhibitor II, EIF2AK2 Inhibitor III, EIF2AK3 Inhibitor II, HRI Inhibitor II, MEKK2 Inhibitor I, PKR Inhibitor III, PKR-like ER Kinase Inhibitor II, BRK Inhibitor II

Primary Target: PERK
504651
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1337532-29-2C₂₃H₂₁FN₆O

Products

Catalogue NumberPackaging Qty/Pack
5046510001 Glass bottle 5 mg
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®
SynonymsEIF2AK1 Inhibitor II, EIF2AK2 Inhibitor III, EIF2AK3 Inhibitor II, HRI Inhibitor II, MEKK2 Inhibitor I, PKR Inhibitor III, PKR-like ER Kinase Inhibitor II, BRK Inhibitor II
References
ReferencesAtkins, C., et al. 2013. Cancer Res. 73, 1993.
Product Information
CAS number1337532-29-2
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
Global Trade Item Number
Catalogue Number GTIN
5046510001 04055977244007

Documentation

PERK Inhibitor II, GSK2656157 - CAS 1337532-29-2 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

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

Brochure

Title
New Products - Antibodies, Assays, Small Molecules, Inhibitors, and Proteins Volume 2, 2014
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
SynonymsEIF2AK1 Inhibitor II, EIF2AK2 Inhibitor III, EIF2AK3 Inhibitor II, HRI Inhibitor II, MEKK2 Inhibitor I, PKR Inhibitor III, PKR-like ER Kinase Inhibitor II, BRK 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
CAS number1337532-29-2
Chemical formulaC₂₃H₂₁FN₆O
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from light
-20°C
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.