[CAS NO. 487021-52-3] AR-A014418
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PRODUCTS SPECIFICATIONS [487021-52-3]
Store
Catalog
SLK-S7435
Brand
Selleck
CAS
487021-52-3
DESCRIPTION [487021-52-3]
Overview
| MDL | MFCD08277040 |
|---|---|
| Molecular Weight | 308.31 |
| Molecular Formula | C12H12N4O4S |
| SMILES | O=C(NC1=NC=C([N+]([O-])=O)S1)NCC2=CC=C(OC)C=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
AR-A014418 (GSK-3β Inhibitor VIII) is an ATP-competitive, and selective inhibitor with and of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested.
Features
Cell-permeable GSK3-selective inhibitor.
In vitro
AR-A014418 inhibits tau phosphorylation at a GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human four-repeat tau protein with IC50 of 2.7 μM, and protects cultured N2A cells from death induced by blocking PI3K/PKB pathway. In hippocampal slices, AR-A014418 inhibits neurodegeneration mediated by beta-amyloid peptide. While in NGP and SH-5Y-SY cells, AR-A014418 reduces neuroendocrine markers and suppresses neuroblastoma cell growth.
In vivo
In ALS mouse model with the G93A mutant human SOD1, AR-A014418 (0-4 mg/kg, i.p.) delays the onset of symptoms, improves motor activity, slows down disease progression, and postpons the endpoint of the disease. In addition, AR-A014418 produces inhibition effect on acetic acid- and formalin-induced nociception in mice by modulating NMDA and metabotropic receptor signaling as well as TNF-α and IL-1β transmission in the spinal cord.
References
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