AR-A014418
Synonym(s):N-(4-Methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea
- Empirical Formula: C12H12N4O4S
- Molecular Weight: 308.31
What is AR-A014418?
Enzyme inhibitor
This ATP-competitive protein kinase inhibitor (FW = 308.31 g/mol; CAS 487021-52-3; Solubility: 62 mg/mL DMSO; <1 mg/mL H2O) selectively targets glycogen synthase kinase 3β (GSK3β),with IC50 = 104 nM; Ki = 38 nM. Attesting to its high specificity for GSK3, AR-A014418 does not significantly inhibit Cdk2 or Cdk5 (IC50 > 100 μM) or 26 other kinases. AR-A014418 inhibits phosphorylation of the microtubule-associated protein Tau at Ser-396 (i.e., the GSK3-specific site) in cells stably expressing human four-repeat Tau. AR-A014418 protects N2A neuroblastoma cells against cell death mediated by inhibition of the phosphatidylinositol 3-kinase/protein kinase B survival pathway. AR- A014418 inhibits neurodegeneration mediated by b-amyloid peptide in hippocampal slices. Treatment of neuroblastoma cell lines with AR- A014418 reduced the level of GSK-3α phosphorylation at Tyr-279 compared to GSK-3β phosphorylation at Tyr-216, and attenuated growth via the maintenance of apoptosis.. AR-A014418-dependent antinociceptive effects are induced by modulation of the glutamatergic system through metabotropic and ionotropic (NMDA) receptors and the inhibition of TNF-α and IL-1β cytokine signaling.
Safety information for AR-A014418
New Products
(S)-3-Aminobutanenitrile hydrochloride 4-Methylphenylacetic acid N-Boc-D-alaninol N-BOC-D/L-ALANINOL Tert-butyl bis(2-chloroethyl)carbamate 3-Morpholino-1-(4-nitrophenyl)-5,6-dihydropyridin- 2(1H)-one Furan-2,5-Dicarboxylic Acid Tropic acid 1-Bromo-3,5-Di-Tert-Butylbenzene S-2-CHLORO PROPIONIC ACID ETHYL ISOCYANOACETATE 2-Bromo-1,3-Bis(Dimethylamino)Trimethinium Hexafluorophosphate 4-IODO BENZOIC ACID 3-NITRO-2-METHYL ANILINE 1-(2,4-DICHLOROPHENYL) ETHANAMINE (2-Hydroxyphenyl)acetonitrile 4-Bromopyrazole 2-(Cyanocyclohexyl)acetic acid 4-methoxy-3,5-dinitropyridine 1-(4-(aminomethyl)benzyl)urea hydrochloride 2-aminopropyl benzoate hydrochloride diethyl 2-(2-((tertbutoxycarbonyl)amino) ethyl)malonate tert-butyl 4- (ureidomethyl)benzylcarbamate Ethyl-2-chloro((4-methoxyphenyl)hydrazono)acetateYou may like
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