GSK2656157

GSK2656157 Basic information
Product Name:GSK2656157
Synonyms:GSK2656157;5-[4-Fluoro-1-[(6-methyl-2-pyridinyl)acetyl]-2,3-dihydro-1H-indol-5-yl]-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine;1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethanone;5-[4-Fluoro-1-[(6-methyl-2-pyridinyl)acetyl]-2,3-dihydro-1H-indol-5-yl]-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine GSK2656157;1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyrid;GSK2656157(GSK-2656157);GSK2656157; GSK 2656157; GSK-2656157.;1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethan-1-one GSK2656157
CAS:1337532-29-2
MF:C23H21FN6O
MW:416.45
EINECS:
Product Categories:Inhibitors
Mol File:1337532-29-2.mol
GSK2656157 Structure
GSK2656157 Chemical Properties
Melting point 194-196°C
Boiling point 744.6±60.0 °C(Predicted)
density 1.43±0.1 g/cm3(Predicted)
storage temp. -20°C
solubility Soluble in DMSO (10 mg/ml with warming)
pka5.32±0.30(Predicted)
form solid
color White
Stability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Safety Information
MSDS Information
GSK2656157 Usage And Synthesis
DescriptionGSK2656157 (1337532-29-2) is a potent (IC50 = 0.9 nM) and selective (over 300 kinases) inhibitor of protein kinase RNA-like endoplasmic reticulum kinase (PERK).1,2? Inhibited growth of multiple human tumor xenografts in mice. GSK2656157 has also been found to potently inhibit RIPK1 (IC50 = 69 nM) and TNF-mediated RIPK1 kinase-dependent cell death in mouse embryonic fibroblasts.3 It prevented the loss of dendritic spines and rescued memory deficits after traumatic brain injury.4? GSK2656157 also enhanced glucose-stimulated insulin secretion in a mouse model of type 2 diabetes mellitus.5
UsesGSK2656157 is an ATP-competitive and highly selective inhibitor of PKR-like endoplasmic reticulum kinase (PERK) enzyme activity. GSK2656157 also has anti-tumor and anti-angiogenic activity.
DefinitionChEBI: GSK2656157 is a pyrrolopyrimidine that is 7-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine which has been substituted at position 5 by a 4-fluoro-2,3-dihydro-1H-indol-5-yl group, the nitrogen of which has been acylated by a (6-methylpyridin-2-yl)acetyl group. An orally bioavailable PERK inhibitor. It has a role as an EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor, a PERK inhibitor and an antineoplastic agent. It is a pyrrolopyrimidine, a biaryl, a member of indoles, a member of methylpyridines, an organofluorine compound and a tertiary carboxamide.
in vivoassay shows that a single 50 mg/kg oral dose of gsk2656157 can completely inhibit the thr980 phosphorylation of endogenous pancreatic perk in mice. furthermore, gsk2656157 causes dose-dependent inhibition of tumor growth in human tumor xenograft models of pancreatic cancer (bxpc3, hpac and capan2) and multiple myeloma (nci-h929). among these cancers, the capan2 tumor is most sensitive [1].
ReferencesAtkins et al. (2013) Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity; Cancer Res. 73 1993 Axten et al. (2014) Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development; ACS Med. Chem. Lett. 4 964 Rojas-Rivera et al. (2017) When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157; Cell Death Differ. 24 1100 Sen et al. (2017) Activation of PERK Elicits Memory Impairment through Inactivation of CREB and Downregulation of PSD95 After Traumatic Brain Injury; Neurosci. 37 5900 Kim et al. (2019) Specific PERK inhibitors enhanced glucose-stimulated insulin secretion in a mouse model of type 2 diabetes; Metabolism, 97 87
GSK2656157 Preparation Products And Raw materials
PLX4032 ISRIB Rapamycin MKC3946 NORFLUOXETINE HYDROCHLORIDE Crizotinib Imiquimod SALUBRINAL PF 573228 MKC8866 7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyriMidin-4-aMine 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide KU57788(NU7441)

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