Molecular Weight(MW): 451.44
GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.
Cited by 16 Publications
7 Customer Reviews
GSK2606414 decreased the number of TUNEL-positive neurons at 72 h after SAH. Representative microphotographs showed the colocalization of NeuN (red) with TUNEL (green)-positive cells in the bilateral basal cerebral cortex at 72 h after SAH (a). Quantitative analysis of TUNEL-positive neurons showed that GSK2606414 decreased the number of apoptotic cells after SAH (b). Scale bar=100 μm, *p < 0.05 versus sham; #p < 0.05 versus SAH + vehicle; ξp < 0.05 versus SAH+GSK2606414 (30 μg).
Mol Neurobiol, 2016, 54(3):1808-1817. GSK2606414 purchased from Selleck.
Representative westerns and summary results showing decreased eIf2α phospho-immunoreactivity (Phos) following intracerebroventricular administration of GSK2606414 (or vehicle) to uninjured mice (n = 4/group). The total levels of eIF2α did not change as a result of treatment. When calculated as a phospho–total ratio (P/T), a significant decrease in phosphorylation was observed in mice treated with GSK2606414. *p < 0.05 between vehicle and drug-treated animals.
J Neurosci, 2018, 38(9):2372-2384. GSK2606414 purchased from Selleck.
C. PERK inhibitor (PERKi, GSK2606414) partially reverted vemurafenib-induced autophagy. BCPAP cells were treated with 5 M PLX and/or 1 M PERKi for 24 hours. After that, protein lysates were prepared and subjected to immunoblotting against the indicated antibodies. Relative quantity of LC3II/LC3I was calculated by ImageJ densitometric analysis and normalized to control (DMSO/DMSO PERKi).
J Clin Endocrinol Metab, 2017, 102(2):634-643. GSK2606414 purchased from Selleck.
(B) PERK inhibitor had no effect on 4-HNE-induced ERK1/2 activation. Cells pretreated with or without the GSK2606414 (10μM, 1h) were treated with 4-HNE as indicated for additional 1h. The protein levels of ERK1/2 and p-ERK1/2 were determined in IEC-6 (left panel) and IPEC-1 cells (right panel).
Sci Rep, 2016, 6:32929. GSK2606414 purchased from Selleck.
A. Recording of the mEPSC amplitude in WT and R451C mice in control conditions or after treatment with GSK2606414. Statistical analysis compares GSK2606414-treated versus vehicletreated control for each genotype. (mean ±SEM; WT ctrl n=11; WT treated n=9, P=0.4158; R451C ctrl n=10; R451C treated n=12, P=0.0304; unpaired t-test). B. The bar-graph shows mEPSC frequency recorded with or without GSK2606414. Statistical analysis compares GSK2606414-treated versus vehicle-treated control for each genotype (mean ±SEM; WT ctrl n=6; WT treated n=9, P=0.5712; R451C ctrl n=10; R451C treated n=12, P=0.0410; unpaired t-test).
Neurobiol Dis, 2018, 120:139-150. GSK2606414 purchased from Selleck.
Purity & Quality Control
Choose Selective PERK Inhibitors
|Description||GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.|
|Features||The first PERK-selective inhibitor with good oral bioavailability and crosses the blood-brain barrier.|
GSK2606414 inhibits PERK Autophosphorylation in A459 Cells with IC50 of <0.3 μM. 
|In vivo||GSK2606414 exhibits high oral availability, and low to moderate blood clearance in mouse, rat, and dog. GSK2606414, administered orally, inhibits tumor growth in a dose-dependent manner in mice bearing pancreatic human BxPC3 tumors. |
|In vitro||DMSO||90 mg/mL (199.36 mM)|
|Ethanol||19 mg/mL (42.08 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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