AR-A014418(GSK3β Inhibitor VIII)

  Cat. No.:  DC7004   Featured
Chemical Structure
487021-52-3
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Field of application
AR-A014418 is a selective and effective GSK3β inhibitor with an IC 50 value of 104 +/- 27 nM; no significant inhibition on 26 other kinases.
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC71176 TC-G 24 TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM.
DC7004 AR-A014418(GSK3β Inhibitor VIII) AR-A014418 is a selective and effective GSK3β inhibitor with an IC 50 value of 104 +/- 27 nM; no significant inhibition on 26 other kinases.
DC1063 TWS119 TWS119 is a GSK-3β inhibitor with IC50 of 30 nM.
DC7680 IM-12 The GSK3β Inhibitor XIX, IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.
DC4227 SB216763 SB 216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).
DC9726 CP21 (CP21R7) CP21R7 is a potent and selective GSK-3β inhibitor.
DC1023 CHIR-99021 (CT99021) CHIR-99021 is a glycogen synthase kinase 3 beta inhibitor that has antiproliferative activity in vitro and in vivo.
DC9703 CHIR-99021 HCl CHIR-99021 HCl is a glycogen synthase kinase 3 beta inhibitor that has antiproliferative activity in vitro and in vivo.
DC7384 CHIR-98014 CHIR-98014 is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.
DC7663 BIO BIO (6-bromoindirubin-3'-oxime) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β, shows >16-fold selectivity over CDK5, also a pan-JAKinhibitor.
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