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

Overview

Key Spec Table

CAS #Empirical Formula
1337531-89-1C₂₄H₂₀F₃N₅O

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516535-5MG
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      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