产品名称

GSK 2606414

产品货号

Axon 2233 CAS [1337531-36-8] MF C24H20F3N5OMW 451.44 Purity: 99% Soluble in DMSO Description Potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK or EIF2AK3) with IC50 value of 0.4 nM and >1000 fold selectivity over EIF2AK1 (HRI) and EIF2AK2 (PKR). Overall, good selectivity was observed, with only 20 protein kinases inhibited >85% by GSK 2606414 at 10 μM during screening against a panel of 294 kinases. It inhibits the growth of a human tumor xenograft in mice with good oral bioavailability and blood-brain barrier penetration.PERK is a type I ER membrane protein and one of three primary effectors of the unfolded protein response (UPR), which has a demonstrated role in tumor growth and angiogenesis. References Certificates Categories Extra info J.M. Axten et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of PERK (...). J. Med. Chem. 2012, 55, 7193-7207. J.A. Moreno et al. Oral Treatment Targeting the Unfolded Protein Response Prevents Neurodegeneration and Clinical Disease in Prion-Infected Mice. Science Translational Medicine 2013, 5(206), 206ra138. Certificate of Analysis Material Safety Data Sheet Angiogenesis Cell Signaling & Oncology PERK EC 2.7.11.1 Potent and selective inhibitor of PERK (EIF2AK3) Chemical name 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone Parent CAS No. [1337531-36-8] Order Size Unit Price Stock 5 mg €99.00 In Stock

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现货询价，电话：010-67529703

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产品品牌

axonmedchem

产品概述

产品详情

GSK 2606414

Based on 18 reference(s) in Google Scholar 9 10 18

Axon 2233

CAS [1337531-36-8]

MF C24H20F3N5O
MW 451.44

Purity: 99%
Soluble in DMSO

GSK 2606414

Description

Potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK or EIF2AK3) with IC50 value of 0.4 nM and >1000 fold selectivity over EIF2AK1 (HRI) and EIF2AK2 (PKR). Overall, good selectivity was observed, with only 20 protein kinases inhibited >85% by GSK 2606414 at 10 μM during screening against a panel of 294 kinases. It inhibits the growth of a human tumor xenograft in mice with good oral bioavailability and blood-brain barrier penetration.PERK is a type I ER membrane protein and one of three primary effectors of the unfolded protein response (UPR), which has a demonstrated role in tumor growth and angiogenesis.

J.M. Axten et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of PERK (...). J. Med. Chem. 2012, 55, 7193-7207.

J.A. Moreno et al. Oral Treatment Targeting the Unfolded Protein Response Prevents Neurodegeneration and Clinical Disease in Prion-Infected Mice. Science Translational Medicine 2013, 5(206), 206ra138.

Potent and selective inhibitor of PERK (EIF2AK3)

Chemical name

1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone

Parent CAS No.

[1337531-36-8]

产品资料