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PI3K/Akt/mTOR signaling GSK-3 AR-A014418

AR-A014418

Catalog No. T1881   CAS 487021-52-3
Synonyms: AR 014418, GSK 3β inhibitor VIII, AR 0133418, GSK-3beta Inhibitor VIII

AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor.

AR-A014418, CAS 487021-52-3
Pack Size Availability Price/USD Quantity
5 mg In stock 50.00
10 mg In stock 59.00
25 mg In stock 102.00
50 mg In stock 185.00
100 mg In stock 320.00
200 mg In stock 416.00
1 mL * 10 mM (in DMSO) In stock 54.00
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Purity 98.00%
Purity 99.94%
Biological Description
Chemical Properties
Storage & Solubility Information
Description AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor.
Targets&IC50 GSK-3β
Kinase Assay 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
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)
Cell lines: N2A cells
Synonyms AR 014418 , GSK 3β inhibitor VIII , AR 0133418 , GSK-3beta Inhibitor VIII
Purity 98.00%
Molecular Weight 308.31
Formula C12H12N4O4S
CAS No. 487021-52-3

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 30.8 mg/mL (100 mM)

Ethanol: 1.5 mg/mL (5 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Bhat R, et al. J Biol Chem. 2003, 278(46), 45937-45945. 2. Carter YM, et al. Cancer Biol Ther. 2014, 15(5). 3. Koh SH, et al. Exp Neurol. 2007, 205(2), 336-346. 4. Martins DF, et al. J Pain. 2011, 12(3), 315-322. 5. Mai C L, Wei X, Gui W S, et al. Differential regulation of GSK-3β in spinal dorsal horn and in hippocampus mediated by interleukin-1beta contributes to pain hypersensitivity and memory deficits following peripheral nerve injury[J]. Molecular pain. 2019, 15: 1744806919826789. 6. Tian J, Li X, Zhao L, et al. Glycyrrhizic Acid Promotes Neural Repair by Directly Driving Functional Remyelination[J]. Food & Function. 2019. 7. Zhang Y, Zhang J, Wang E, et al. Microcystin-Leucine-Arginine Induces Tau Pathology Through Bα Degradation via Protein Phosphatase 2A Demethylation and Associated Glycogen Synthase Kinase-3β Phosphorylation. Toxicological Sciences. 2018, 162(2): 475-487. 8. Zhang Y, Zhang J, Wang E, et al. Microcystin-LR induces tau pathology through Bα degradation via PP2A demethylation and associated GSK-3β phosphorylation[J]. Toxicological Sciences. 2018 Apr 1;162(2):475-487.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Anti-diabetic Compound Library Stem cell Differentiation Compound Library Autophagy Compound Library Neuronal Signaling Compound Library PI3K-AKT-mTOR Compound Library Kinase Inhibitor Library Anti-cancer Metabolism Compound Library Preclinical Compound Library Wnt&Hedgehog&Notch Compound Library Promoting Cancer Cell Differentiation Compound Library Anti-obesity Compound Library Anti-aging Compound Library HIF-1 Signaling Pathway Compound Library Neurodegenerative disease-related Compound Library Anti-Lung Cancer Compound Library Glycometabolism Compound Library Anti-Breast Cancer Compound Library Anti-Pancreatic Cancer Compound Library Anti-Alzheimer's Disease Compound Library

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