Cas No.: | 487021-52-3 |
Chemical Name: | 1-[(4-methoxyphenyl)methyl]-3-(5-nitro-1,3-thiazol-2-yl)urea |
Synonyms: | AR-AO 14418; AR 0133418; AR 014418; GSK 3β inhibitor |
SMILES: | COC1=CC=C(C=C1)CNC(=O)NC2=NC=C(S2)[N+](=O)[O-] |
Formula: | C12H12N4O4S |
M.Wt: | 308.31308 |
Sotrage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
Description: | AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor with an IC50 of 104 nM。 |
In Vivo: | AR-A014418 (0-4 mg/kg, i.p.) delays the onset of symptoms, enhances motor activity, blocks disease progression, and postpons the endpoint of the disease in ALS mouse model with the G93A mutant human SOD1[3]. Furthermore, AR-A014418 suppresses acetic acid- and formalin-induced nociception in mice via modulating NMDA and metabotropic receptor signaling as well as TNF-α and IL-1β transmission in the spinal cord[4]. |
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]. |