Inhibitor of eukaryotic translation initiation factor 2 alpha kinase 3;Inhibitor of myosin light chain kinase 2
Product Description
PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states.
1.Axten JM, Medina JR, Feng Y, Shu A, Romeril SP, Grant SW, Li WH, Heerding DA, Minthorn E, Mencken T et al.. (2012) 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 protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).. J Med Chem, 55 (16):(7193-207). [PMID:22827572][10.1021/op500134e]
2.Moreno JA, Halliday M, Molloy C, Radford H, Verity N, Axten JM, Ortori CA, Willis AE, Fischer PM, Barrett DA et al.. (2013) Oral treatment targeting the unfolded protein response prevents neurodegeneration and clinical disease in prion-infected mice.. Sci Transl Med, 5 (206):(206ra138). [PMID:24107777][10.1021/op500134e]
3.Smith HL, Mallucci GR. (2016) The unfolded protein response: mechanisms and therapy of neurodegeneration.. Brain, 139 (Pt 8):(2113-21). [PMID:27190028][10.1021/op500134e]
4.Axten JM, Romeril SP, Shu A, Ralph J, Medina JR, Feng Y, Li WH, Grant SW, Heerding DA, Minthorn E et al.. (2013) Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.. ACS Med Chem Lett, 4 (10):(964-8). [PMID:24900593][10.1021/op500134e]
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I2413407