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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

Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
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China
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2922
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Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
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China
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6005
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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 17702719238
Email
sales@sun-shinechem.com
Country
China
ProdList
976
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Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
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4727
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58
Chengdu NoVi Biotechnology Co., Ltd.
Tel
028-81458053
Fax
028-81458053
Email
novibiotech@163.com sales@novi-biotech.com
Country
China
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226
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Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
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China
ProdList
7552
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61
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
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4861
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AdooQ BioScience, LLC
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+1 (866) 930-6790
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+1 (866) 333-9607
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info@adooq.com
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United States
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Shanghai Taifu Pharmaceutical Technology Co. LTD
Tel
021-58111238 18930958102
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021-58111238
Email
sales@taifupharm.com
Country
China
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510
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55
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
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60
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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:


  • 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