Chemical Name: 1-[5-(4-Amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethenone
PERK inhibitor
Molecular Weight:
451.44
Purity:
98% by HPLC NMR (Conforms)
Form:
Off-white solid
CAS Number:
[1337531-36-8]
Formula:
C24H20F3N5O
Application Notes:
Potent (IC50 = 0.4 nM) and selective (against a panel of 294 kinases) inhibitor of protein kinase R-like endoplasmic reticulum kinase (PERK), an important effector of the unfolded protein response (UPR).1 It prevented neurodegeneration in a mouse model of frontotemporal dementia2 and rodent models of Parkinsons disease via modulation of the UPR3. GSK2606414 has been reported to be a potent inhibitor of RIPK1 (IC50 = 18 nM).4 It has also displayed neuroprotective effects in various models of stroke.5-7
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