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Postion:Product Catalog >Biochemical Engineering>Inhibitors>PI3K / Akt / mTOR>GSK-3 inhibitors>AR-A014418
AR-A014418
  • AR-A014418

AR-A014418 NEW

Price $45 $53 $91
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: AR-A014418 CAS No.: 487021-52-3
Purity: ≥95% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameAR-A014418
DescriptionAR-A014418 (GSK 3β inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor.
Cell ResearchCell 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)
Kinase AssayGSK3 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.
In vitroAR-A014418 inhibited neuroendocrine markers and inhibited the growth of neuroma cells in NGP cells and SH-5Y-SY cells.AR-A014418 inhibited neurodegeneration induced by β-like amyloid peptide in hippocampal slices.AR-A014418 inhibited the expression of tau in 3T3 fibroblasts expressing human four-repeat tau proteins at the GSK3-specific locus (Ser AR-A014418 inhibited tau phosphorylation at the GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human tetra-repeat tau protein with an IC50 of 2.7 μM and protected cultured N2A cells from death induced by blocking the PI3K/PKB pathway.
In vivoAR-A014418 inhibited neuroendocrine markers and inhibited the growth of neuroma cells in NGP cells and SH-5Y-SY cells.AR-A014418 inhibited neurodegeneration induced by β-like amyloid peptide in hippocampal slices.AR-A014418 inhibited the expression of tau in 3T3 fibroblasts expressing human four-repeat tau proteins at the GSK3-specific locus (Ser AR-A014418 inhibited tau phosphorylation at the GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human tetra-repeat tau protein with an IC50 of 2.7 μM and protected cultured N2A cells from death induced by blocking the PI3K/PKB pathway.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : 1.5 mg/mL (5 mM)
DMSO : 30.8 mg/mL (100 mM)
KeywordsAR-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-A 014418 | AR014418 | AR-A014418 | GSK-3 | ARA014418 | GSK 3b inhibitor VIII
Inhibitors RelatedPHA-767491 | Cromolyn sodium | GSK 3 Inhibitor IX | CHIR-99021 | AT7519 | 5-Bromoindole | 4-Chloro-2'-bromoacetophenone | SNS-032 | CHIR-99021 HCl | GSK-3 Inhibitor 5 | MeBIO | 1-Azakenpaullone
Related Compound LibrariesHighly Selective Inhibitor Library | Anti-Colorectal Cancer Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Metabolism Compound Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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