ChemicalBook > CAS DataBase List > AR-A014418

AR-A014418

Product Name
AR-A014418
CAS No.
487021-52-3
Chemical Name
AR-A014418
Synonyms
CS-1021;SN 4521;AR 014418;AR 0133418;AR-AO 14418;AR-A014418-D3;GSK 3β inhibitor;AR-A014418, >=98%;AR-A014418 (SN-4521;AR-A014418/ARA014418
CBNumber
CB9497883
Molecular Formula
C12H12N4O4S
Formula Weight
308.31
MOL File
487021-52-3.mol
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AR-A014418 Property

Melting point:
208-210?C (dec.)
Density 
1.464±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: ≥20mg/mL, clear, light yellow
pka
5.80±0.70(Predicted)
form 
Yellow solid
color 
off-white to tan
Sensitive 
Light Sensitive
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
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Safety

Hazard Codes 
Xn
Risk Statements 
22-37/38-41
Safety Statements 
26-36/39
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H318Causes serious eye damage

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P405Store locked up.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
A3230
Product name
AR-A014418
Purity
≥98% (HPLC), solid
Packaging
5mg
Price
$206
Updated
2024/03/01
Sigma-Aldrich
Product number
361549
Product name
GSK-3β Inhibitor VIII
Packaging
5mg
Price
$159
Updated
2024/03/01
Alfa Aesar
Product number
J64554
Product name
GSK-3beta Inhibitor VIII
Packaging
10mg
Price
$187
Updated
2023/06/20
Cayman Chemical
Product number
14704
Product name
GSK3β Inhibitor VIII
Purity
≥98%
Packaging
5mg
Price
$72
Updated
2024/03/01
Cayman Chemical
Product number
14704
Product name
GSK3β Inhibitor VIII
Purity
≥98%
Packaging
10mg
Price
$135
Updated
2024/03/01
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AR-A014418 Chemical Properties,Usage,Production

Description

AR-A 014418 (487021-52-3) is a selective glycogen synthase kinase 3 (GSK-3) inhibitor, IC50 = 104 nM. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices. Anti-inflammatory activity. Cell permeable. Active in rodent models.

Chemical Properties

Pale Yellow Solid

Uses

AR-A014418 has been used as an inhibitor of glycogen synthase kinase 3 (GSK3).

Uses

Glycogen Synthase Kinase 3β (GSK-3β) inhibitor.

General Description

A cell-permeable thiazole-containing urea compound that acts as a potent inhibitor of GSK-3. Shown to inhibit GSK-3β with high potency (IC50 = 104 nM). Inhibition is competitive with respect to ATP (Ki = 38 nM). Specificity has been reported using a panel of 28 different kinases, including Cdk2 and Cdk5 (IC50 >100 μM). Shown to prevent tau phosphorylation at a GSK-3-specific site. Also shown to protect neuronal cells against Aβ-mediated neurodegeneration in vitro and reduce tauopathy in mice in vivo (30 μmol/kg delivered with 40% PEG400 and 40% dimethylacetamide in water). Caution: Do not use delivering vehicles containing dimethylamine for in vivo studies, as it is highly toxic to animals. A 25 mM (5 mg/649 μl) solution of GSK-3β Inhibitor VIII (Cat. No. 361557) in DMSO is also available.

Biochem/physiol Actions

Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimer′s disease. GSK3 inhibitor, AR-A014418, inhibits GSK3 (IC50 = 104 nM), in an ATP-competitive manner (Ki = 38 nM). AR-A014418 does not significantly inhibit cdk2 or cdk5 (IC50 > 100 μM) or 26 other kinases, demonstrating high specificity for GSK3.

in vitro

ara014418 acted as an atp-competitive manner and did not significantly inhibit cdk2 or cdk5 or 26 other kinases demonstrating high specificity for gsk3. ar-a014418 inhibited tau phosphorylation at a gsk3-specific site (ser-396) in cells stably expressing human four-repeat tau protein [1].

in vivo

ara014418 induced behavioural changes that were consistent with the effects of antidepressant drugs. subacute intraperitoneal injections of ar-a014418 reduced immobility time in rats exposed to the forced swim test, which was a well-established model for antidepressant efficacy. moreover, the specificity of this effect was supported by our finding that ar-a014418 decreased spontaneous as well as amphetamine-induced activity [2].

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.

IC 50

104 ± 27 nm

storage

+4°C

References

1) Bhat et al. (2003), Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418; J. Biol. Chem., 278 45937 2) Ramirez et al. (2010), Inhibition of glycogen synthase kinase 3beta (GSK3β) decreases inflammatory responses in brain endothelial cells; Am. J. Pathol., 176 881

AR-A014418 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from AR-A014418 manufacturers

Career Henan Chemical Co
Product
AR-A014418 487021-52-3
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-23

487021-52-3, AR-A014418Related Search:

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  • GSK-3β Inhibitor VIII - CAS 487021-52-3 - Calbiochem
  • AR-A014418(GSK3β Inhibitor VIII)
  • CS-1021
  • AR-AO 14418; AR 0133418; AR 014418; GSK 3Β INHIBITOR
  • AR-A014418-D3
  • AR 0133418;GSK 3Β INHIBITOR VIII;AR 014418
  • N-(4-Methoxybenzyl)-N'-(5-nitro-1,3-thiazol-2-yl)urea AR 0133418
  • AR 0133418
  • GSK 3B Inhibitor VIII
  • AR 014418
  • GSK 3β inhibitor
  • 1-(4-Methoxybenzyl)-3-(5-nitrothiazol-2-yl)urea
  • AR-A014418/ARA014418
  • SN 4521
  • AR-A014418, >=98%
  • N-[(4-Methoxyphenyl)methyl]-N'-(5-nitro-2-thiazolyl)urea
  • N-[(4-Methoxyphenyl)Methyl]-N'-(5-nitro-thiazol-2-yl)urea
  • AR-AO 14418
  • GSK-3β Inhibitor VIII
  • Urea, N-[(4-methoxyphenyl)methyl]-N'-(5-nitro-2-thiazolyl)-
  • GSK3β Inhibitor VIII
  • 1-(4-Methoxybenzyl)-3-(5-nitrothiazol-2-yl)ure
  • AR-A014418(GSK3βInhibitorVIII)
  • AR-A014418 (SN-4521
  • 1-[(4-methoxyphenyl)methyl]-3-(5-nitro-1,3-thiazol-2-yl)urea
  • 487021-52-3
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  • Intermediates & Fine Chemicals