1337531-89-1 Usage
Uses
Used in Pharmaceutical Industry:
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 is used as a potential therapeutic agent for the treatment of various diseases. Its application is based on its ability to modulate specific biological pathways and target proteins, making it a promising candidate for drug development.
Used in Cancer Treatment:
In the field of oncology, this compound is used as an inhibitor of PERK, an important transmembrane protein of the endoplasmic reticulum (ER). It has potential use in the treatment of various types of cancer, including breast, colon, pancreatic, and lung cancers. By targeting PERK, this compound may help in modulating the unfolded protein response pathways, which are often dysregulated in cancer cells.
Used in Treatment of Neurodegenerative Diseases:
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 also has potential applications in the treatment of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis. Its ability to target PERK and modulate the unfolded protein response pathways may contribute to its therapeutic effects in these conditions.
Used in Treatment of Cardiovascular Diseases:
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 is also used in the treatment of cardiovascular diseases, including myocardial infarction, atherosclerosis, and arrhythmias. Its role in modulating the unfolded protein response pathways may help in addressing the underlying cellular stress and dysfunction associated with these conditions.
Used in Ocular Disease Treatment:
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 has potential applications in the treatment of ocular diseases. Its ability to target PERK and modulate the unfolded protein response pathways may help in addressing the cellular stress and dysfunction associated with various eye conditions.
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).
Check Digit Verification of cas no
The CAS Registry Mumber 1337531-89-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,3,7,5,3 and 1 respectively; the second part has 2 digits, 8 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1337531-89:
(9*1)+(8*3)+(7*3)+(6*7)+(5*5)+(4*3)+(3*1)+(2*8)+(1*9)=161
161 % 10 = 1
So 1337531-89-1 is a valid CAS Registry Number.
1337531-89-1Relevant articles and documents
COMPOUNDS AND METHODS FOR TREATING INSULIN RESISTANCE SYNDROME
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, (2014/08/19)
The present invention relates to a method of treating or preventing insulin resistance syndrome in an animal body by administering an inhibitor of protein kinase RNA-like endoplasmic reticulum kinase (PERK) gene, or a functional variant thereof, or an inhibitor of PERK protein or a functional variant thereof or a method of reducing activity of transcription factors of the FOXO family (Foxo 1, 3a, 4 and 6) by administering an inhibitor of protein kinase RNA-like endoplasmic reticulum kinase (PERK) gene, or a functional variant thereof, or an inhibitor of PERK protein or a functional variant thereof. The present invention also relates to different compounds and methods for using PERK gene or PERK protein.
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro- 1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK)
Axten, Jeffrey M.,Medina, Jesús R.,Feng, Yanhong,Shu, Arthur,Romeril, Stuart P.,Grant, Seth W.,Li, William Hoi Hong,Heerding, Dirk A.,Minthorn, Elisabeth,Mencken, Thomas,Atkins, Charity,Liu, Qi,Rabindran, Sridhar,Kumar, Rakesh,Hong, Xuan,Goetz, Aaron,Stanley, Thomas,Taylor, J. David,Sigethy, Scott D.,Tomberlin, Ginger H.,Hassell, Annie M.,Kahler, Kirsten M.,Shewchuk, Lisa M.,Gampe, Robert T.
, p. 7193 - 7207 (2012/11/07)
Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in tumori-genesis and cancer cell survival stim
