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GSK2656157

GSK2656157 Structure
GSK2656157 structure
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;GSK2656157, 10 mM in DMSO;PERK Inhibitor II, GSK2656157;4-Dihydroxybenzoic acid methyl ester
CBNumber:
CB62664486
Molecular Formula:
C23H21FN6O
Molecular Weight:
416.45
MDL Number:
MFCD27997885
MOL File:
1337532-29-2.mol
MSDS File:
SDS
Last updated:2025-10-21 14:56:34
Product description Number Pack Size Price
PERK Inhibitor II, GSK2656157 5.04651 5 mg $215
GSK2656157 ≥98% 17372 5mg $47
GSK2656157 ≥98% 17372 10mg $87
GSK2656157 ≥98% 17372 25mg $206
GSK2656157 ≥98% 17372 50mg $360
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GSK2656157 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)
pka 5.32±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.
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P264-P270-P301+P312-P330-P501
NFPA 704
0
2 0

GSK2656157 price More Price(31)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 5.04651 PERK Inhibitor II, GSK2656157 1337532-29-2 5 mg $215 2025-07-31 Buy
Cayman Chemical 17372 GSK2656157 ≥98% 1337532-29-2 5mg $47 2024-03-01 Buy
Cayman Chemical 17372 GSK2656157 ≥98% 1337532-29-2 10mg $87 2024-03-01 Buy
Cayman Chemical 17372 GSK2656157 ≥98% 1337532-29-2 25mg $206 2024-03-01 Buy
Cayman Chemical 17372 GSK2656157 ≥98% 1337532-29-2 50mg $360 2024-03-01 Buy
Product number Packaging Price Buy
5.04651 5 mg $215 Buy
17372 5mg $47 Buy
17372 10mg $87 Buy
17372 25mg $206 Buy
17372 50mg $360 Buy

GSK2656157 Chemical Properties,Uses,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].

IC 50

EIF2AK3 (PERK): 0.9 nM (IC50); EIF2AK1 (HRI): 460 nM (IC50); BRK: 905 nM (IC50); EIF2AK2 (PKR): 905 nM (IC50); MEKK3: 954 nM (IC50); Aurora B: 1259 nM (IC50); KHS: 1764 nM (IC50); LCK: 2344 nM (IC50); MLK2: 2796 nM (IC50); MEKK3: 2847 nM (IC50); ALK5: 3020 nM (IC50); MLCK2: 3039 nM (IC50); EIF2AK4(GCN2): 3162 nM (IC50); c-MER: 3431 nM (IC50); PI3Kγ: 3802 nM (IC50); WNK3: 5951 nM (IC50); LRRK2: 6918 nM (IC50); ROCK1: 7244 nM (IC50); MSK1: 8985 nM (IC50); NEK1: 9807 nM (IC50); AXL: 9808 nM (IC50); JAK2: 24547 nM (IC50)

References

[1] CHARITY ATKINS. Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity.[J]. Cancer research, 2013, 73 6: 1993-2002. DOI:10.1158/0008-5472.can-12-3109
[2] JEFFREY M. AXTEN*. Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development[J]. ACS Medicinal Chemistry Letters, 2013, 4 10: 964-968. DOI:10.1021/ml400228e
[3] DIEGO ROJAS-RIVERA. When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157[J]. Cell Death and Differentiation, 2017, 24 6: 1100-1110. DOI:10.1038/cdd.2017.58
[4] TANUSREE SEN. Activation of PERK Elicits Memory Impairment through Inactivation of CREB and Downregulation of PSD95 After Traumatic Brain Injury.[J]. Journal of Neuroscience, 2017, 37 24: 5900-5911. DOI:10.1523/jneurosci.2343-16.2017
[5] MIN JOO KIM . Specific PERK inhibitors enhanced glucose-stimulated insulin secretion in a mouse model of type 2 diabetes[J]. Metabolism: clinical and experimental, 2019, 97: Pages 87-91. DOI:10.1016/j.metabol.2018.12.007

GSK2656157 Preparation Products And Raw materials

Raw materials

Preparation Products

GSK2656157 Suppliers

Global( 119)Suppliers
Supplier Tel Email Country ProdList Advantage
Hubei Jusheng Technology Co.,Ltd. 		18871490254 linda@hubeijusheng.com CHINA 28172 58
career henan chemical co 		+86-0371-86658258 +8613203830695 factory@coreychem.com China 29799 58
Zhengzhou Alfa Chemical Co.,Ltd 		+8618530059196 sale04@alfachem.cn China 11945 58
TargetMol Chemicals Inc. 		+1-781-999-5354; +17819995354 marketing@targetmol.com United States 32435 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6312 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1026@dideu.com China 20287 58
InvivoChem 		+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58
HANGZHOU LEAP CHEM CO., LTD. 		+86-571-87711850 market18@leapchem.com China 24727 58
ShenZhen Trendseen Biological Technology Co.,Ltd. 		13417589054 trendseenbio@gmail.com China 11681 58
Aladdin Scientific 		tp@aladdinsci.com United States 57505 58
Supplier Advantage
Hubei Jusheng Technology Co.,Ltd. 		58
career henan chemical co 		58
Zhengzhou Alfa Chemical Co.,Ltd 		58
TargetMol Chemicals Inc. 		58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		58
Dideu Industries Group Limited 		58
InvivoChem 		58
HANGZHOU LEAP CHEM CO., LTD. 		58
ShenZhen Trendseen Biological Technology Co.,Ltd. 		58
Aladdin Scientific 		58

View Lastest Price from GSK2656157 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
GSK2656157 pictures 2025-10-20 GSK2656157
1337532-29-2
 US $30.00-74.00 / mg 99.80% 10g TargetMol Chemicals Inc.
GSK2656157 pictures 2020-01-14 GSK2656157
1337532-29-2
 US $1.00 / g 1g 99% 200kg Career Henan Chemical Co
  • GSK2656157 pictures
  • GSK2656157
    1337532-29-2
  • US $30.00-74.00 / mg
  • 99.80%
  • TargetMol Chemicals Inc.
  • GSK2656157 pictures
  • GSK2656157
    1337532-29-2
  • US $1.00 / g
  • 99%
  • Career Henan Chemical Co

GSK2656157 Spectrum

GSK2656157(1337532-29-2)1HNMR

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MKC3946 ISRIB 7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyriMidin-4-aMine PF 573228 SALUBRINAL
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1of3

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 GSK2656157, 10 mM in DMSO PERK Inhibitor II, GSK2656157 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 1337532-29-2 C23H21FN6O Inhibitors