1337531-89-1 Usage
Chemical Properties
Pale Yellow Solid
Uses
Different sources of media describe the Uses of 1337531-89-1 differently. You can refer to the following data:
1. 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.
2. 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.
3. 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.
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.
