AR-A014418
![AR-A014418 Structure](CAS/GIF/487021-52-3.gif)
- 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
- MOL File:
- 487021-52-3.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/7/12 16:43:06
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. |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() ![]() GHS05,GHS07 |
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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(3)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich(India) | A3230 | AR-A014418 ≥98% (HPLC), solid | 487021-52-3 | 5MG | ₹16421.53 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | A3230 | AR-A014418 ≥98% (HPLC), solid | 487021-52-3 | 25MG | ₹65675.28 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | 361549 | GSK-3β Inhibitor VIII - CAS 487021-52-3 - Calbiochem The GSK-3β Inhibitor VIII, also referenced under CAS 487021-52-3, controls the biological activity of GSK-3β. This small molecule/inhibitor is primari | 487021-52-3 | 5MG | ₹16670.01 | 2022-06-14 | Buy |
AR-A014418 Chemical Properties,Uses,Production
Chemical Properties
Pale Yellow Solid
Uses
AR-A014418 has been used as an inhibitor of glycogen synthase kinase 3 (GSK3).
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.
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.
AR-A014418 Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32836 | 60 | Inquiry |
career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29888 | 58 | Inquiry |
BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | United States | 19892 | 58 | Inquiry |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10522 | 58 | Inquiry |
InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
Coresyn Pharmatech Co., Ltd. | +86-571-86626709 +86-18157142896 | China | 9991 | 58 | Inquiry |
Supplier | Advantage |
---|---|
CLEARSYNTH LABS LTD. | 58 |
A.J Chemicals | 58 |
ATK CHEMICAL COMPANY LIMITED | 60 |
career henan chemical co | 58 |
BOC Sciences | 58 |
Chongqing Chemdad Co., Ltd | 58 |
TargetMol Chemicals Inc. | 58 |
Zhejiang J&C Biological Technology Co.,Limited | 58 |
InvivoChem | 58 |
Coresyn Pharmatech Co., Ltd. | 58 |
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