GSK2606414

Catalog No.S7307

GSK2606414 Chemical Structure

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.

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USD 197 In stock
USD 870 In stock
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Cited by 12 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.

    Representative images from a TUNEL assay of labeled apoptotic cells in control and RCN1-knockdown HepG2 cells treated with TM (8 μm, 48 h) in the presence or absence of GSK2606414 (2 μm, 1 h) treatment. Scale bar, 50 μm.

    Oncogenesis, 2017, 6(3):e304. GSK2606414 purchased from Selleck.

  • A representative picture of western blotting for PERK and EIF2A using mouse islets according to the concentrations of GSK2606414, and the quantitative analyses (n = 3).

    J Endocrinol, 2018, 236(3):125-136. GSK2606414 purchased from Selleck.

Purity & Quality Control

Choose Selective PERK Inhibitors

Biological Activity

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.
Targets
EIF2AK3 (PERK) [1]
(Cell-free assay)
0.4 nM
In vitro

GSK2606414 inhibits PERK Autophosphorylation in A459 Cells with IC50 of <0.3 μM. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A549 cells MXXGeY5kfGmxbjDhd5NigQ>? NWLQOmp7OiCq M3O2cmlvcGmkaYTpc44hd2ZidHjhdJNq\2G{Z3nuMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckBw\iCSRWLLJIlvKGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgNkBpenNiYomgW4V{fGW{bjDicI91fGmwZx?= NF[zPXkzOjh{N{W3Ni=>
human A549 cells MX\GeY5kfGmxbjDhd5NigQ>? M2m4NlAvODNizszN NYjLfVBYOiCq M{PvNmlvcGmkaYTpc44hd2ZidHjhdJNq\2G{Z3nuMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckBw\iCSRWLLJIlvKGi3bXHuJGE2PDliY3XscJMh[XRiMD6wN{B2VSCjZoTldkAzKGi{czDifUBY\XO2ZYLuJIJtd3S2aX7n MV[yNlgzPzV5Mh?=
human A549 cells M2fwZmZ2dmO2aX;uJIF{e2G7 Ml;mNUBp M2mxXGlvcGmkaYTpc44hd2ZidHjhdJNq\2G{Z3nuMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckBw\iCSRWLLJIlvKGi3bXHuJGE2PDliY3XscJMheHKnaX7jeYJifGWmIH\vdkAyKGi{IH\vcIxwf2WmIHL5JJRp[XC|aXfhdodqdi2rbnT1Z5Rqd25ibXXhd5Vz\WRiYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3S2aX7nJIFv[Wy7c3nz MX6yOFkxODV7Mx?=

... Click to View More Cell Line Experimental Data

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. [1]

Protocol

Animal Research:

[1]

+ Expand
  • Animal Models: BxPC3 human pancreatic xenograft model
  • Formulation: 0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in water
  • Dosages: ~150 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (199.36 mM)
Ethanol 19 mg/mL (42.08 mM)
Water Insoluble
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.
20mg/mL

* 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.

Chemical Information

Molecular Weight 451.44
Formula

C24H20F3N5O

CAS No. 1337531-36-8
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID