Cat. No. Name Size Price Add Cart
KI3733AR-A01441810 mg$164
AR-A01441850 mg$460

Chemical Characteristic

Product NameAR-A014418
CAS No.487021-52-3
Molecular Weight 308.32
FormulaC12H12N4O4S
Chemical NameN-(4-Methoxybenzyl)-N'-(5-nitro-1,3-thiazol-2-yl)urea
SmilesN(C(=O)Nc1sc(cn1)[N](=O)O)Cc1ccc(cc1)OC
Chemical Structure

Biological activities

AR-A014418 is a selective and effective GSK3? inhibitor with an IC 50 value of 104 +/- 27 nM. It has no significant inhibition on other 26 kinases [1]. 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 ?M, and protects cultured N2A cells from death induced by blocking PI3K/PKB pathway [2]. In vivo, it can be used by 0-4 mg/kg in ALS mouse model. 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-? and IL-1? transmission in the spinal cord [3].

References

[1] Bhat R, Xue Y, Berg S, et al. Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J Biol Chem. 2003, 278(46):45937-45945.
[2] Min HJ, Koh SS, Cho IR, Inhibition of GSK-3beta enhances reovirus-induced apoptosis in colon cancer cells. Int J Oncol. 2009, 35(3):617-624. [3] Gould TD, Einat H, Bhat R, AR-A014418, a selective GSK-3 inhibitor, produces antidepressant-like effects in the forced swim test. Int J Neuropsychopharmacol. 2004 , 7(4):387-390.

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