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Tideglusib

AOB5562

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$10.00

$10.00 per mg

Quantity Discount Table - Order More To Get More Price Discount

QuantitymgUnit Price ($/mg or $/Unit)Final Price
15 $8.50 Total: $42.50
110 $7.20 Total: $72.00
125 $6.10 Total: $152.50
150 $5.20 Total: $260.00
1100 $4.50 Total: $450.00

Data sheet

Molecular FormulaC19H14N2O2S
Molecular Weight334.39
CAS Numbers865854-05-3
Storage Condition0°C (short term), -20°C (long term), desiccated
SolubilityDMSO
Purity98% by HPLC
SynonymNP031112; NP 031112; NP-031112; Tideglusib.
IUPAC/Chemical Name2-(1-naphthalenyl)-4-(phenylmethyl)-1,2,4-thiadiazolidine-3,5-dione
InChl KeyPMJIHLSCWIDGMD-UHFFFAOYSA-N
InChl CodeInChI=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
SMILES CodeO=C(N1CC2=CC=CC=C2)N(C3=C4C=CC=CC4=CC=C3)SC1=O
References1) Koros C, Stamelou M. Interventions in progressive supranuclear palsy. Parkinsonism Relat Disord. 2015 Sep 25. pii: S1353-8020(15)00424-1. doi: 10.1016/j.parkreldis.2015.09.033. [Epub ahead of print] PubMed PMID: 26459661.

2) Sun A, Li C, Chen R, Huang Y, Chen Q, Cui X, Liu H, Thrasher JB, Li B. GSK-3β controls autophagy by modulating LKB1-AMPK pathway in prostate cancer cells. Prostate. 2015 Oct 6. doi: 10.1002/pros.23106. [Epub ahead of print] PubMed PMID: 26440826.

More info

Tideglusib (also known as NP031112 or NP-12) is a potent, irreversible, non-ATP-competitive inhibitor of glycogen synthase kinase-3 beta (GSK-3β). GSK-3β is a serine/threonine kinase involved in various cellular processes, including cell cycle regulation, apoptosis, and gene expression. By inhibiting GSK-3β, Tideglusib modulates these pathways, offering therapeutic potential in several diseases.Wikipedia+3Wiley Online Library+3selleck.co.jp+3


Mechanism of Action

Tideglusib binds covalently to the cysteine residue (Cys199) in the active site of GSK-3β, leading to irreversible inhibition. This binding prevents GSK-3β from phosphorylating its substrates, thereby altering downstream signaling pathways. Unlike ATP-competitive inhibitors, Tideglusib's non-ATP-competitive nature allows for selective targeting of GSK-3β without affecting other kinases with similar ATP-binding sites.MDPI


Clinical Applications and Research

1. Neurological Disorders

  • Alzheimer's Disease (AD): Tideglusib has been evaluated in clinical trials for AD, aiming to reduce tau hyperphosphorylation and amyloid plaque formation. However, these trials were discontinued due to lack of efficacy .PubMed+1Wikipedia+1

  • Progressive Supranuclear Palsy (PSP): Similar to AD, trials for PSP were halted for the same reasons.

  • Amyotrophic Lateral Sclerosis (ALS): Ongoing studies are investigating Tideglusib's potential in ALS treatment, focusing on its neuroprotective effects.

2. Myotonic Dystrophy

Tideglusib is under investigation for treating congenital and childhood-onset myotonic dystrophy type I. Early-phase trials suggest potential benefits in improving muscle function, but further research is needed .ClinicalTrials.gov+4Wikipedia+4Wikipedia+4

3. Other Applications

  • Tooth Repair: Preclinical studies indicate that Tideglusib may promote dentine formation, suggesting potential applications in dental tissue regeneration.Frontiers

  • Cancer Research: Investigations into Tideglusib's effects on neuroblastoma and ovarian cancer cells have shown promise in inducing apoptosis through reactive oxygen species (ROS) pathways.

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