AR-A014418
- CAS No.
- 487021-52-3
- Chemical Name:
- AR-A014418
- Synonyms
- SN 4521;CS-1021;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
- Molecular Weight:
- 308.31
- MDL Number:
- MFCD08277040
- MOL File:
- 487021-52-3.mol
- MSDS File:
- SDS
| 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 |
| form | Yellow solid |
| pka | 5.80±0.70(Predicted) |
| 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. |
| FDA UNII | 87KSH90Q6D |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS05,GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H302-H315-H318-H335 | |||||||||
| Precautionary statements | P261-P280-P305+P351+P338-P280a-P304+P340-P405-P501a | |||||||||
| Hazard Codes | Xn | |||||||||
| Risk Statements | 22-37/38-41 | |||||||||
| Safety Statements | 26-36/39 | |||||||||
| WGK Germany | 3 | |||||||||
| NFPA 704 |
|
AR-A014418 price More Price(33)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | A3230 | AR-A014418 ≥98% (HPLC), solid | 487021-52-3 | 5mg | $206 | 2024-03-01 | Buy |
| Sigma-Aldrich | 361549 | GSK-3β Inhibitor VIII | 487021-52-3 | 5mg | $159 | 2024-03-01 | Buy |
| Alfa Aesar | J64554 | GSK-3beta Inhibitor VIII | 487021-52-3 | 10mg | $187 | 2023-06-20 | Buy |
| Cayman Chemical | 14704 | GSK3β Inhibitor VIII ≥98% | 487021-52-3 | 5mg | $72 | 2024-03-01 | Buy |
| Cayman Chemical | 14704 | GSK3β Inhibitor VIII ≥98% | 487021-52-3 | 10mg | $135 | 2024-03-01 | Buy |
AR-A014418 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| Shanghai Zheyan Biotech Co., Ltd. | 18017610038 | zheyansh@163.com | CHINA | 3620 | 58 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Coresyn Pharmatech Co., Ltd. | +86-571-86626709 +86-18157142896 | cbc@coresyn.com | China | 9991 | 58 |
View Lastest Price from AR-A014418 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2019-07-06 | AR-A014418
487021-52-3
|
US $2.00 / kg | 1kg | 99% | 100kg | Career Henan Chemical Co |
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- AR-A014418
487021-52-3
- US $2.00 / kg
- 99%
- Career Henan Chemical Co