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AR-A014418

Catalog No. T1881 CAS 487021-52-3

Synonyms: AR 0133418, GSK-3beta Inhibitor VIII, AR 014418, GSK 3β inhibitor VIII

AR-A014418 (GSK 3β inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

AR-A014418, CAS 487021-52-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 45.00
10 mg	In stock	$ 53.00
25 mg	In stock	$ 91.00
50 mg	In stock	$ 166.00
100 mg	In stock	$ 288.00
200 mg	In stock	$ 373.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.94%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AR-A014418 (GSK 3β inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor.
Targets&IC50	GSK-3β:38 nM(Ki)
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 (&sim;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)

Synonyms	AR 0133418, GSK-3beta Inhibitor VIII, AR 014418, GSK 3β inhibitor VIII
Molecular Weight	308.31
Formula	C12H12N4O4S
CAS No.	487021-52-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 1.5 mg/mL (5 mM)

DMSO: 30.8 mg/mL (100 mM)

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.

Citations

1. Zhang Y, Zhang J, Wang E, et al. Microcystin-LR induces tau pathology through Bα degradation via PP2A demethylation and associated GSK-3β phosphorylation. Toxicological Sciences. 2018 Apr 1;162(2):475-487 2. 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 3. Tian J, Li X, Zhao L, et al. Glycyrrhizic Acid Promotes Neural Repair by Directly Driving Functional Remyelination. Food & Function. 2019 4. 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. Molecular pain. 2019, 15: 1744806919826789.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Anti-Neurodegenerative Disease Compound Library Kinase Inhibitor Library Autophagy Compound Library Wnt/Hedgehog/Notch Compound Library Glycolysis Compound Library Metabolism Compound Library Cancer Cell Differentiation Compound Library Anti-Diabetic Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AR-A014418 487021-52-3 PI3K/Akt/mTOR signaling Stem Cells GSK-3 AR-A-014418 AR A014418 GSK-3b Inhibitor VIII Glycogen synthase kinase 3 Inhibitor GSK-3β Inhibitor VIII GSK 3beta inhibitor VIII AR-0133418 inhibit AR0133418 Glycogen synthase kinase-3 AR-014418 AR 0133418 AR-A 014418 AR014418 GSK-3beta Inhibitor VIII AR 014418 GSK 3β inhibitor VIII ARA014418 GSK 3b inhibitor VIII inhibitor

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