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Submit ReviewAR-A 014418
Description: Selective GSK-3 inhibitor
Chemical Name: N-[(4-Methoxyphenyl)methyl]-N'-(5-nitro-2-thiazolyl)urea
Purity: ≥99% (HPLC)
Biological Activity for AR-A 014418
AR-A 014418 is a selective glycogen synthase kinase 3 (GSK-3) inhibitor (IC50 = 104 nM). Exhibits specificity for GSK-3 over cdk2 and cdk5 (IC50 values are > 100 μM) and over 26 other kinases. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices.
Licensing Information
Sold with the permission of AstraZeneca UK Ltd.
Compound Libraries for AR-A 014418
AR-A 014418 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for AR-A 014418
| M. Wt | 308.31 |
| Formula | C12H12N4O4S |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 487021-52-3 |
| PubChem ID | 448014 |
| InChI Key | YAEMHJKFIIIULI-UHFFFAOYSA-N |
| Smiles | O=C(NCC2=CC=C(OC)C=C2)NC1=NC=C([N+]([O-])=O)S1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AR-A 014418
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 30.83 | 100 | |
| ethanol | 1.54 | 5 |
Preparing Stock Solutions for AR-A 014418
The following data is based on the product molecular weight 308.31. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.24 mL | 16.22 mL | 32.43 mL |
| 5 mM | 0.65 mL | 3.24 mL | 6.49 mL |
| 10 mM | 0.32 mL | 1.62 mL | 3.24 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.65 mL |
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Product Datasheets for AR-A 014418
References for AR-A 014418
References are publications that support the biological activity of the product.
Bhat and Budd (2002) GSK3β signalling: casting a wide net in Alzheimer's disease. Neurosignals 11 251 PMID: 12566926
Bhat et al (2003) Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J.Biol.Chem. 278 45937 PMID: 12928438
Gould et al (2004) AR-A014418, a selective GSK-3 inhibitor, produces antidepressant-like effects in the forced swim test. Int.J.Neuropsychopharmacol. 7 387 PMID: 15315719
If you know of a relevant reference for AR-A 014418, please let us know.
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Keywords: AR-A 014418, AR-A 014418 supplier, ARA014418, glycogen, synthase, kinase, 3, GSK-3, GSK3, inhibitors, inhibits, Glycogen, Synthase, Kinase, 3966, Tocris Bioscience
4 Citations for AR-A 014418
Citations are publications that use Tocris products. Selected citations for AR-A 014418 include:
Ling et al (2019) Interleukin-1β drives NEDD8 nuclear-to-cytoplasmic translocation, fostering parkin activation via NEDD8 binding to the P-ubiquitin activating site. J Neuroinflammation 16 275 PMID: 31882005
Penas et al (2015) GSK3 inhibitors stabilize Wee1 and reduce cerebellar granule cell progenitor proliferation. Tuberc Respir Dis (Seoul) 14 417 PMID: 25616418
Cuesto et al (2015) GSK3β Inhibition Promotes Synaptogenesis in Drosophila and Mammalian Neurons. PLoS One 10 e0118475 PMID: 25764078
Chen et al (2012) Spatially coordinated kinase signaling regulates local axon degeneration. J Neurosci 32 13439 PMID: 23015435
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Pathways for AR-A 014418
