516535 Sigma-AldrichPERK Inhibitor I, GSK2606414 - CAS 1337531-89-1 - Calbiochem
PERK 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 reg
More>> PERK 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. Less<<MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Synonyms: DDR2 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
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Overview
Key Spec Table
| CAS # | Empirical Formula |
|---|---|
| 1337531-89-1 | C₂₄H₂₀F₃N₅O |
Products
| Catalogue Number | Packaging | Qty/Pack | |
|---|---|---|---|
| 516535-5MG | Glass bottle | 5 mg |
| Description | |
|---|---|
| Overview | A 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 Number | 516535 |
| Brand Family | Calbiochem® |
| Synonyms | DDR2 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 | |
|---|---|
| References | Moreno, 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 number | 1337531-89-1 |
| Form | White powder |
| Hill Formula | C₂₄H₂₀F₃N₅O |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ200 |
| Biological Information | |
|---|---|
| Primary Target | Perk |
| Primary Target IC<sub>50</sub> | 0.4 nM against EIF2AK3/PERK-catalyzed EIF2&alpha |
| Purity | ≥99% by HPLC |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 516535-5MG | 04055977198126 |