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
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.
Safety
- Hazard Codes
- Xn
- Risk Statements
- 22-37/38-41
- Safety Statements
- 26-36/39
- WGK Germany
- 3
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.
N-Bromosuccinimide Price
- Product number
- A3230
- Product name
- AR-A014418
- Purity
- ≥98% (HPLC), solid
- Packaging
- 5mg
- Price
- $206
- Updated
- 2024/03/01
- Product number
- 361549
- Product name
- GSK-3β Inhibitor VIII
- Packaging
- 5mg
- Price
- $159
- Updated
- 2024/03/01
- Product number
- J64554
- Product name
- GSK-3beta Inhibitor VIII
- Packaging
- 10mg
- Price
- $187
- Updated
- 2023/06/20
- Product number
- 14704
- Product name
- GSK3β Inhibitor VIII
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $72
- Updated
- 2024/03/01
- Product number
- 14704
- Product name
- GSK3β Inhibitor VIII
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $135
- Updated
- 2024/03/01
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
- Product
- AR-A014418 487021-52-3
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-12-23