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516535 PERK Inhibitor I, GSK2606414 - CAS 1337531-89-1 - Calbiochem

516535
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Overview

Key Spec Table

CAS #Empirical Formula
1337531-89-1C₂₄H₂₀F₃N₅O

Products

Catalogue NumberPackaging Qty/Pack
516535-5MG Glass bottle 5 mg
Description
OverviewA cell-permeable pyrrolopyrimidamine compound that acts as a highly potent EIF2AK3/PERK inhibitor (IC50 = 0.4 nM; [ATP] = 5 µM) by targeting PERK in its inactive DFG conformation at the ATP-binding region, while displaying ≥385-fold selectivity over c-Kit, Aurora B, BRK, HRI/EIF2AK1, MLK2/MAP3K10, c-MER, DDR2, PKR/EIF2AK2, and MLCK2/MYLK2 (IC50 = 154, 407, 412, 420, 452, 474, 524, 696, and 701 nM, respectively) and little activity against more than 280 other kinases (IC50 >1 µM). Shown to block ER stress-induced PERK autophosphorylation following Thapsigargin (Cat. No. 586005) addition in A549 cultures in vitro (by 100% at ≤30 nM; 60 min preincubation) and effectively retard PxBC-3 tumor growth in mice in vivo (50 and 150 mg/kg/12 h p.o.). Also available as a 25 mM solution in DMSO (Cat. No. 508340).
Catalogue Number516535
Brand Family Calbiochem®
SynonymsDDR2 Inhibitor I, EIF2AK1 Inhibitor I, EIF2AK2 Inhibitor II, HRI Inhibitor I, MLCK Inhibitor VI, MLK2/MAP3K10 Inhibitor I, PKR-like ER Kinase Inhibitor I, Aurora Kinase Inhibitor IX, BRK Inhibitor I, c-Kit Inhibitor III, Mer RTK Inhibitor II, EIF2AK3 Inhibitor I, PKR Inhibitor II, MERTK Inhibitor II, RP38 Inhibitor II, TAM Family RTK Inhibitor II, Double-stranded RNA-activated Protein Kinase Inhibitor II, Double-stranded RNA-dependent Protein Kinase Inhibitor II, 7-Methyl-5-(1-((3-trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone
References
ReferencesMoreno, J.A., et al. 2013. Sci Transl. Med.<\i> 5, 1.
Axten, J.M., et al. 2012. J. Med. Chem. 55, 7193.
Product Information
CAS number1337531-89-1
FormWhite powder
Hill FormulaC₂₄H₂₀F₃N₅O
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ200
Applications
ApplicationPERK Inhibitor I, GSK2606414, CAS 1337531-89-1, is a cell-permeable, highly potent EIF2AK3/PERK inhibitor (IC50 = 0.4 nM) that targets PERK in its inactive DFG conformation at the ATP-binding region.
Biological Information
Primary TargetPerk
Primary Target IC<sub>50</sub>0.4 nM against EIF2AK3/PERK-catalyzed EIF2&alpha
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
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
Global Trade Item Number
Catalogue Number GTIN
516535-5MG 04055977198126