GSK2656157

Product Name: GSK2656157
CAS No.: 1337532-29-2
Chemical Name: GSK2656157
Synonyms: 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;CS-804;GSK2656157;GSK2656157 USP/EP/BP;GSK2656157(GSK-2656157);PERK inhibitor GS2656157;PERK inhibitor GSK2656157;4-Dihydroxybenzoic acid methyl ester;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-methylpyrid
CBNumber: CB62664486
Molecular Formula: C23H21FN6O
Formula Weight: 416.45
MOL File: 1337532-29-2.mol

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GSK2656157 Property

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)
form: solid
pka: 5.32±0.30(Predicted)
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.

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 17372
Product name: GSK2656157
Purity: ≥98%
Packaging: 5mg
Price: $47
Updated: 2024/03/01

Cayman Chemical

Product number: 17372
Product name: GSK2656157
Purity: ≥98%
Packaging: 10mg
Price: $87
Updated: 2024/03/01

Cayman Chemical

Product number: 17372
Product name: GSK2656157
Purity: ≥98%
Packaging: 25mg
Price: $206
Updated: 2024/03/01

Cayman Chemical

Product number: 17372
Product name: GSK2656157
Purity: ≥98%
Packaging: 50mg
Price: $360
Updated: 2024/03/01

TRC

Product number: G797515
Product name: GSK2656157
Packaging: 100mg
Price: $725
Updated: 2021/12/16

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GSK2656157 Chemical Properties,Usage,Production

Description

GSK2656157 (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

Uses

GSK2656157 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.

Definition

ChEBI: 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 vivo

assay 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].

References

Atkins 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

Raw materials

Preparation Products

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GSK2656157 Suppliers

China 81 India 2 United States 15 Global 98

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View Lastest Price from GSK2656157 manufacturers

Career Henan Chemical Co

Product: GSK2656157 1337532-29-2
Price: US $1.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 200kg
Release date: 2020-01-13

1337532-29-2, GSK2656157Related Search:

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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

PERK inhibitor GS2656157

CS-804

Ethanone, 1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydro-1H-indol-1-yl]-2-(6-methyl-2-pyridinyl)-

GSK2656157 USP/EP/BP

PERK inhibitor GSK2656157

4-Dihydroxybenzoic acid methyl ester

1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydroindol-1-yl]-2-(6-methylpyridin-2-yl)ethanone

1337532-29-2

C23H21FN6O

Inhibitors