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> AR-A014418 [487021-52-3]

AR-A014418 [487021-52-3]

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Referencia HY-10512-10mg

embalaje : 10mg

Marca : MedChemExpress

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Descripciòn

AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM)[1].

IC50 & Target[1]

GSK-3β

104 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
BXPC-3 IC50
14 μM
Compound: 77, AR-A014418
Growth inhibition of human BxPC3 cells after 72 hrs by MTS assay
Growth inhibition of human BxPC3 cells after 72 hrs by MTS assay
[PMID: 19338355]
HuP-T3 IC50
22 μM
Compound: 77, AR-A014418
Growth inhibition of human HUPT3 cells after 72 hrs by MTS assay
Growth inhibition of human HUPT3 cells after 72 hrs by MTS assay
[PMID: 19338355]
MIA PaCa-2 IC50
29 μM
Compound: 77, AR-A014418
Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay
Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay
[PMID: 19338355]
Sf21 IC50
0.104 μM
Compound: AR-A014418
Inhibition of recombinant full length human GSK3beta expressed in Sf21 insect cells using biotinylated-AAEELDSRAGS(PO3H2)PQL peptide as substrate preincubated enzyme-substrate mixture for 15 to 20 mins followed by [gamma-33P]ATP addition and measured afte
Inhibition of recombinant full length human GSK3beta expressed in Sf21 insect cells using biotinylated-AAEELDSRAGS(PO3H2)PQL peptide as substrate preincubated enzyme-substrate mixture for 15 to 20 mins followed by [gamma-33P]ATP addition and measured afte
[PMID: 32435391]
In Vitro

AR-A014418 blocks the phosphorylation of tau at a GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human four-repeat tau protein, with an IC50 of 2.7 μM, and protects cultured N2A cells from death cuased by PI3K/PKB pathway blockage. AR-A014418 also shows inhibitory effect on neurodegeneration mediated by beta-amyloid peptide in hippocampal slices[1].
AR-A014418 decreases neuroendocrine markers and suppresses neuroblastoma cell growth in NGP and SH-5Y-SY cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AR-A014418 Related Antibodies

Solvente y solubilidad
In Vitro: 

DMSO : ≥ 100 mg/mL (324.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2435 mL 16.2174 mL 32.4349 mL
5 mM 0.6487 mL 3.2435 mL 6.4870 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Pureza y Documentación
Referencias

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