GSK2606414 | PERK inhibitor

CAS:
 1337531-36-8
Catalog Number:
 10-4716
GSK2606414 supplier | CAS 1337531-36-8 | Focus Biomolecules

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GSK2606414 (1337531-36-8) is a 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).It has also displayed neuroprotective effects in various models of stroke.5-7

References/Citations:

  1. Axten 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]pyrimidine-4-amine (GSK2606414); J. Med. Chem., 55 7193
  2. Radford et al. (2015), PERK inhibition prevents tau-mediated neurodegeneration in a mouse model of frontotemporal dementia; Acta Neuropathol., 130 633
  3. Mercado et al. (2018), Targeting PERK signaling with the small molecules GSK2606414 prevents neurodegeneration in a model of Parkinson’s disease; Neurobiol. Dis., 112 136
  4. 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
  5. Yan et al. (2017), Pharmacological Inhibition of PERK Attenuates Early Brain Injury After Subarachnoid Hemorrhage in Rats Through the Activation of Akt; Mol. Neurobiol., 54 1808
  6. Meng et al. (2018), PERK Pathway Activation Promotes Intracerebral Hemorrhage Induced Secondary Brain Injury by Inducing Apoptosis Both in Vivo and in Vitro; Front. Neurosci., 12 111
  7. Dhir et al. (2023), PERK inhibitor, GSK2606414, ameliorates neuropathological damage, memory and motor functional impairments in cerebral ischemia via PERK/p-eIFα/ATP/CHOP signaling; Metab. Brain Dis., online ahead of print
CAS:
1337531-36-8
Catalog Number:
10-4716
Activity:
PERK inhibitor
Chemical Names:
1-[5-(4-Amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethenone
Molecular Weight:
451.44
Molecular Formula:

C24H20F3N5O

Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white solid
Purity:

98% HPLC
NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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