1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone
- Product Name
- 1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone
- CAS No.
- 1337531-89-1
- Chemical Name
- 1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone
- Synonyms
- PERK-IN-4;PERK Inhibitor I;GSK PERK Inhibitor;PERK Inhibitor I, GSK2606414;1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-fluoro-5-(trifluoromethyl)phenyl)ethanone;1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-fluoro-5-(trifluoromethyl)phenyl)ethan-1-one;1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone;Ethanone, 1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoromethyl)phenyl]-
- CBNumber
- CB52620944
- Molecular Formula
- C24H19F4N5O
- Formula Weight
- 469.43
- MOL File
- 1337531-89-1.mol
1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone Property
- Melting point:
- 233-238°C (dec.)
- storage temp.
- -20C
- solubility
- DMSO (Slightly), Methanol (Slightly, Heated)
- form
- White powder
- color
- Off-White to Pale Yellow
N-Bromosuccinimide Price
- Product number
- 516535
- Product name
- PERK Inhibitor I, GSK2606414 - CAS 1337531-89-1 - Calbiochem
- Packaging
- 5mg
- Price
- $207
- Updated
- 2025/07/31
- Product number
- G797800
- Product name
- GSKPERKInhibitor
- Packaging
- 10mg
- Price
- $285
- Updated
- 2021/12/16
- Product number
- 278359
- Product name
- GSK PERK inhibitor
- Packaging
- 1mg
- Price
- $408
- Updated
- 2021/12/16
- Product number
- G797800
- Product name
- GSKPERKInhibitor
- Packaging
- 50mg
- Price
- $1040
- Updated
- 2021/12/16
- Product number
- FG23705
- Product name
- GSK PERK inhibitor
- Packaging
- 5mg
- Price
- $300
- Updated
- 2021/12/16
1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone Chemical Properties,Usage,Production
Chemical Properties
Pale Yellow Solid
Uses
GSK PERK Inhibitor is an inhibitor of PERK, an important transmembrane protein of endoplasmic reticulum (ER). GSK PERK Inhibitor can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways. As a result, GSK PERK Inhibitor has potential use in the treatment of diseases such as Alzheimer''s disease, stroke, Type 1 diabetes, Parkinson disease, Huntington''s disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung.
Uses
GSK PERK Inhibitor is an inhibitors of PERK, an important transmembrane protein of endoplasmic reticulum (ER). GSK PERK Inhibitor can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways. As a result, GSK PERK Inhibitor has potential use in the treatment of diseases such as Alzheimer's disease, stroke, Type 1 diabetes, Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung.
Biological Activity
Cell permeable: yes', 'Primary Target
Perk', 'Reversible: yes', 'Target IC50: 0.4 nM against EIF2AK3/PERK-catalyzed EIF2&alpha
Enzyme inhibitor
This first-in-class, orally bioavailable pyrrolopyrimidamine and smallmolecule protein kinase inhibitor (FW = 449.42 g/mol; CAS 1337531-89-1; Soluble in DMSO; Cell Permeable), also known by its code name GSK- 2606414 (or GSK2606414), its systematic name 7-methyl-5-(1-((3- trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3- d]pyrimidin-4-amine, and by many aliases, targets the protein kinase R (PKR)-like endoplasmic reticulum kinase, or PERK, IC50 = 0.4 nM, a key transducer of the unfolded protein response, or UPR. Primary Mode of Inhibition: Accumulation of unfolded proteins within the ER elicits release of ER chaperones from the stress-sensing domain of PERK. Once activated by oligomerization and autophosphorylation, PERK phosphorylates Ser-51 of eukaryotic initiation factor 2α (eIF2α), thereby inhibiting overall protein synthesis and providing time for the ER to clear itself of accumulated unfolded proteins. PERK Inhibitor I blocks ER stress-induced PERK autophosphorylation (nearly 100% inhibition at ≤30 nM after 30 min) after thapsigargin treatment (See Thapsigargin) of A549 cultures in vitro and effectively retards PxBC-3 tumor growth in mice in vivo. Other Target(s): c-Kit (IC50 = 150 nM), Aurora B (IC50 = 410 nM), BRK (IC50 = 410 nM), HRI/EIF2AK1 (IC50 = 420 nM), MLK2/MAP3K10 (IC50 = 450 nM), c-MER (IC50 = 470 nM), DDR2 (IC50 = 520 nM), PKR/EIF2AK2 (IC50 = 700 nM), and MLCK2/MYLK2 (IC50 = 700 nM), with little activity against more than 280 other kinases (IC50 >1 μM).
1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone Preparation Products And Raw materials
Raw materials
Preparation Products
1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone Suppliers
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