AR-A014418, >=98% (HPLC), solid
Application
AR-A014418 has been used as an inhibitor of glycogen synthase kinase 3 (GSK3).
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.
Features and Benefits
This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
This compound is featured on the PKB/Akt page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
General description
AR-A014418 may have chronic pain-relieving properties. In mice having neuropathic pain, this molecule has been shown to have antihyperalgesic effects. AR-A014418 may modulate proinflammatory cytokines and the catecholaminergic and serotonergic pathways. It has also been studied that AR-A014418 inhibits growth of pancreatic cancer cells.
Packaging
5 mg in glass bottle
| Colour | off-white to tan |
|---|---|
| Quality Level | 100 |
| InChI key | YAEMHJKFIIIULI-UHFFFAOYSA-N |
| InChI | 1S/C12H12N4O4S/c1-20-9-4-2-8(3-5-9)6-13-11(17)15-12-14-7-10(21-12)16(18)19/h2-5,7H,6H2,1H3,(H2,13,14,15,17) |
| Manufacturer | SIGMA-ALDRICH |
| Form | solid |
| Assay | ≥98% (HPLC) |
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