AR-A014418

Catalog No.S7435 Synonyms: GSK-3β Inhibitor VIII

AR-A014418 Chemical Structure

Molecular Weight(MW): 308.31

AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested.

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USD 270 In stock
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1 Customer Review

  • Protein levels of p-GSK3α/β (Tyr279/Tyr216, Ser21/Ser9) and total GSK3α/β in A549 cells with Lithium chloride, SB216763, TWS119 or ARA014418 treatment were assessed by immunoblotting

    Cell Physiol Biochem, 2017, 42(3):1177-1191. AR-A014418 purchased from Selleck.

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Biological Activity

Description AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested.
Features Cell-permeable GSK3-selective inhibitor.
Targets
GSK-3β [1]
(Cell-free assay)
GSK-3β [1]
(Cell-free assay)
38 nM(Ki) 38 nM(Ki)
In vitro

AR-A014418 inhibits tau phosphorylation at a GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human four-repeat tau protein with IC50 of 2.7 μM, and protects cultured N2A cells from death induced by blocking PI3K/PKB pathway. In hippocampal slices, AR-A014418 inhibits neurodegeneration mediated by beta-amyloid peptide. [1] While in NGP and SH-5Y-SY cells, AR-A014418 reduces neuroendocrine markers and suppresses neuroblastoma cell growth. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human BxPC3 cells M{HCZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfPO|IhcA>? NWTSfJZ7T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSniSQ{OgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NF0yPCEQvF2= NFTL[2syQTN|OEO1OS=>
human HUPT3 cells M4XS[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnvaO|IhcA>? MnrIS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTHVRXDNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhUUN3ME2yNkDPxE1? M3K5VlE6OzN6M{W1
human MIAPaCa2 cells NUPGOlVbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUK3NkBp NGXoXolIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOUUGSYVPhNkBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTTJIF{e2G7LDDJR|UxRTJ7IN88US=> M2LT[FE6OzN6M{W1

... Click to View More Cell Line Experimental Data

In vivo In ALS mouse model with the G93A mutant human SOD1, AR-A014418 (0-4 mg/kg, i.p.) delays the onset of symptoms, improves motor activity, slows down disease progression, and postpons the endpoint of the disease. [3] In addition, AR-A014418 produces inhibition effect on acetic acid- and formalin-induced nociception in mice by modulating NMDA and metabotropic receptor signaling as well as TNF-α and IL-1β transmission in the spinal cord. [4]

Protocol

Kinase Assay:

[1]

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GSK3 Scintillation Proximity Assay:

The competition experiments are carried out in duplicate with 10 concentrations of the inhibitor in clear-bottomed microtiter plates. The biotinylated peptide substrate, biotin-AAEELDSRAGS(PO3H2)PQL, is added at a final concentration of 2 μM in an assay buffer containing 6 milliunits of recombinant human GSK3 (equal mix of both α and β), 12 mM MOPS, pH 7.0, 0.3 mM EDTA, 0.01% β-mercaptoethanol, 0.004% Brij 35, 0.5% glycerol, and 0.5 μg of bovine serum albumin/25 μl and preincubated for 10-15 min. The reaction is initiated by the addition of 0.04 μCi of [γ-33P]ATP and unlabeled ATP in 50 mM Mg(Ac)2 to a final concentration of 1 μM ATP and assay volume of 25 μl. Blank controls without peptide substrate are used. After incubation for 20 min at room temperature, each reaction is terminated by the addition of 25 μl of stop solution containing 5 mM EDTA, 50 μM ATP, 0.1% Triton X-100, and 0.25 mg of streptavidin-coated SPA beads corresponding to ∼35 pmol of binding capacity. After 6 h the radioactivity is determined in a liquid scintillation counter. Inhibition curves are analyzed by non-linear regression using GraphPad Prism.
Cell Research:

[1]

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  • Cell lines: N2A cells
  • Concentrations: ~50 μM
  • Incubation Time: 24 h
  • Method:

    Cell viability is assessed by calcein/propidium iodide uptake. Calcein AM is taken up and cleaved by esterases present within living cells, yielding yellowish-green fluorescence, whereas PI is only taken up by dead cells, which become orange-red fluorescent. In brief, N2A cells are cultured for 2 days in vitro and then treated with 50 μM LY-294002 in the presence of AR-A014418 or vehicle (DMSO) for 24 h. Subsequently, N2A cells are incubated for 30 min with 2 μM PI and 1 μM calcein-AM. The cultures are then rinsed three times with Hanks' buffered saline solution containing 2 mM CaCl2, and the cells are visualized by fluorescence microscopy using a Zeiss Axiovert 135 microscope. Three fields (selected at random) are analyzed per well (∼300 cells/field) in at least three different experiments. Cell death is expressed as percentage of PI-positive cells from the total number of cells. In every experiment, specific cell death is obtained after subtracting the number of dead cells present in vehicle-treated cultures.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: ALS mouse model with the G93A mutant human SOD1
  • Formulation: Normal saline
  • Dosages: ~4 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (197.85 mM)
Water Insoluble
Ethanol Insoluble

* 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 308.31
Formula

C12H12N4O4S

CAS No. 487021-52-3
Storage powder
Synonyms GSK-3β Inhibitor VIII

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID