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Merck

SML0339

Tideglusib

≥98% (HPLC), glycogen synthase kinase-3 inhibitor, powder

Sinónimos:

4-Benzyl-2-(naphthalen-1-yl)-[1,2,4]thiadiazolidine-3,5-dione, NP-12, NP031112

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Fórmula empírica (notación de Hill):
C19H14N2O2S
Número CAS:
Peso molecular:
334.39
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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Nombre del producto

Tideglusib, ≥98% (HPLC)

Quality Segment

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)

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 is a potent non ATP-competitive inhibitor of glycogen synthase kinase-3 (GSK3).
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.


Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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