SML0339

Tideglusib

≥98% (HPLC)

• Synonym(s): 4-Benzyl-2-(naphthalen-1-yl)-[1,2,4]thiadiazolidine-3,5-dione, NP-12, NP031112
• Empirical Formula (Hill Notation): C₁₉H₁₄N₂O₂S
• CAS Number: 865854-05-3
• Molecular Weight: 334.39
• MDL number: MFCD18633296
• UNSPSC Code: 12352200
• PubChem Substance ID: 329825344
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: >15 mg/mL
• storage temp.: 2-8°C
• SMILES string: O=C1SN(C(=O)N1Cc2ccccc2)c3cccc4ccccc34
• InChI: 1S/C19H14N2O2S/c22-18-20(13-14-7-2-1-3-8-14)19(23)24-21(18)17-12-6-10-15-9-4-5-11-16(15)17/h1-12H,13H2
• InChI key: PMJIHLSCWIDGMD-UHFFFAOYSA-N
• Gene Information: human ... GSK3B(2932)

Description

Application

Tideglusib has been used:

• as a reference compound in ADP-GloTM Kinase assay
• as an allosteric inhibitor of GSK-3β to study its effects on myocardial remodeling and angiogenesis
• as a differentiation agent (specifically a glycogen synthase kinase (GSK)-3β inhibitor) to convert fibroblast cells into octamer-binding transcription factor-4 (OCT4)+ and vascular endothelial growth factor receptor-2 (VEGFR-2/fetal liver kinase-1 (FLK1)+ cells

Biochem/physiol Actions

Tideglusib, also known as NP031112 or NP-12, is a potent non ATP-competitive inhibitor of glycogen synthase kinase-3 (GSK3), an important kinase studied in stem cell research and neurodegenerative diseases. It is currently in clinical trials for Alzheimer′s disease and Progressive Supranuclear Palsy (PSP). Tideglusib reduces phosphorylation of the tau protein and the accumulation of amyloid plaques, reduces hippocampal and entorhinal cortex neuron loss and improves spatial memory deficits. It has also shown neuroprotective and anti-inflammatory activity in a variety of animal models.

Features and Benefits

This compound is featured on the GSK-3 page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable