| 產(chǎn)品名稱 | GSK 2606414 |
| 產(chǎn)品貨號(hào) | 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 |
| 產(chǎn)品價(jià)格 | 現(xiàn)貨詢價(jià)，電話：010-67529703 |
| 產(chǎn)品規(guī)格 | |
| 產(chǎn)品品牌 | axonmedchem |
| 產(chǎn)品概述 | |
| 產(chǎn)品詳情 |
GSK 2606414Axon 2233 CAS [1337531-36-8] MF C24H20F3N5O
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.
Potent and selective inhibitor of PERK (EIF2AK3)
Chemical name1-(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] |
| 產(chǎn)品資料 |
