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GSK2656157

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;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

Molecular Weight:: 416.45

MDL Number:: MFCD27997885

MOL File:: 1337532-29-2.mol

MSDS File:: SDS

Last updated:2024-11-19 23:02:33

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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)
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.

SAFETY

Risk and Safety Statements

Symbol(GHS)

GHS07

Signal word

Warning

Hazard statements

H302

Precautionary statements

P264-P270-P301+P312-P330-P501

NFPA 704

	0
2		0

GSK2656157 price More Price(30)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	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
TRC	G797515	GSK2656157	1337532-29-2	100mg	$725	2021-12-16	Buy

Product number	Packaging	Price	Buy
17372	5mg	$47	Buy
17372	10mg	$87	Buy
17372	25mg	$206	Buy
17372	50mg	$360	Buy
G797515	100mg	$725	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].

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

GSK2656157 Suppliers

Global( 98)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	29811	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32161	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	22785	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6391	58
LEAP CHEM CO., LTD.	+86-852-30606658	market18@leapchem.com	China	24727	58
ShenZhen Trendseen Biological Technology Co.,Ltd.	13417589054	trendseenbio@gmail.com	China	11681	58
Aladdin Scientific	+1-+1(833)-552-7181	sales@aladdinsci.com	United States	57505	58
Amadis Chemical Company Limited	571-89925085	sales@amadischem.com	China	131957	58

Supplier	Advantage
Hubei Jusheng Technology Co.,Ltd.	58
career henan chemical co	58
TargetMol Chemicals Inc.	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	58
Dideu Industries Group Limited	58
InvivoChem	58
LEAP CHEM CO., LTD.	58
ShenZhen Trendseen Biological Technology Co.,Ltd.	58
Aladdin Scientific	58
Amadis Chemical Company Limited	58

View Lastest Price from GSK2656157 manufacturers

Image	Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
	2024-11-19	GSK2656157 1337532-29-2	US $32.00-74.00 / mg		99.89%	10g	TargetMol Chemicals Inc.
	2020-01-14	GSK2656157 1337532-29-2	US $1.00 / g	1g	99%	200kg	Career Henan Chemical Co

GSK2656157
1337532-29-2
US $32.00-74.00 / mg
99.89%
TargetMol Chemicals Inc.

GSK2656157
1337532-29-2
US $1.00 / g
99%
Career Henan Chemical Co

GSK2656157 Spectrum

GSK2656157(1337532-29-2)¹HNMR

1337532-29-2(GSK2656157)Related Search:

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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 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 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-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