Tideglusib

Name: Tideglusib
Brand: AOBIOUS
SKU: AOB5562
Price: 13 USD
Availability: InStock

Cat No: AOB5562

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Quantity Discount Table - Order More To Get More Price Discount

Quantity	mg	Unit Price ($/mg or $/Unit)	Final Price
1	5	$8.50	Total: $42.50
1	10	$7.20	Total: $72.00
1	25	$6.10	Total: $152.50
1	50	$5.20	Total: $260.00
1	100	$4.50	Total: $450.00

Overview

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.

Chemical Properties

Molecular Formula	C19H14N2O2S
Molecular Weight	334.39
CAS Numbers	865854-05-3
Solubility	DMSO
Purity	98% by HPLC
IUPAC/Chemical Name	2-(1-naphthalenyl)-4-(phenylmethyl)-1,2,4-thiadiazolidine-3,5-dione
InChl Key	PMJIHLSCWIDGMD-UHFFFAOYSA-N
InChl Code	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
SMILES Code	O=C(N1CC2=CC=CC=C2)N(C3=C4C=CC=CC4=CC=C3)SC1=O

Storage and Handling

0°C (short term), -20°C (long term), desiccated

Synonyms

NP031112; NP 031112; NP-031112; Tideglusib.

References

1) 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.