SB-245570

Chemical compound

SB-245570
INN
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CAS Number	209481-36-7
PubChem	9829145
DrugBank
ChemSpider	8004820
KEGG

SB-245570 is a chemical compound that acts as a potent and selective inhibitor of the enzyme glycogen synthase kinase 3 (GSK-3). It is primarily used in scientific research to study the role of GSK-3 in various cellular processes and diseases.

Chemical Structure and Properties

Chemical structure of SB-245570

SB-245570 is characterized by its pyrrole-2,5-dione core structure, which is substituted with a 3,4-dimethoxyphenyl group and a 4-fluorophenyl group. The presence of these substituents contributes to its high affinity and selectivity for GSK-3.

The molecular formula of SB-245570 is C₁₈H₁₄FNO₄, and it has a molecular weight of approximately 327.31 g/mol. The compound is typically synthesized through a series of organic reactions involving the formation of the pyrrole ring and subsequent functionalization.

Mechanism of Action

SB-245570 inhibits GSK-3 by binding to the ATP-binding site of the enzyme, thereby preventing the phosphorylation of its substrates. GSK-3 is a serine/threonine kinase involved in numerous cellular processes, including glycogen metabolism, cell cycle regulation, and apoptosis. By inhibiting GSK-3, SB-245570 can modulate these pathways, making it a valuable tool for studying the enzyme's role in various biological contexts.

Applications in Research

SB-245570 is widely used in biomedical research to investigate the physiological and pathological roles of GSK-3. It has been employed in studies related to neurodegenerative diseases, such as Alzheimer's disease, where GSK-3 is implicated in the formation of tau protein tangles and amyloid-beta plaques. Additionally, SB-245570 has been used to explore the potential therapeutic effects of GSK-3 inhibition in cancer, diabetes, and bipolar disorder.

Pharmacological Effects

In preclinical studies, SB-245570 has demonstrated the ability to cross the blood-brain barrier, making it suitable for investigating central nervous system effects. Its selective inhibition of GSK-3 has been shown to result in neuroprotective effects, reduction of inflammation, and modulation of insulin signaling.

Safety and Toxicity

As with many research chemicals, the safety and toxicity profile of SB-245570 in humans is not well-established, as it is primarily used in laboratory settings. Researchers handling SB-245570 should follow standard safety protocols for handling chemical reagents.

Related Pages

• Glycogen synthase kinase 3
• Neurodegenerative diseases
• Alzheimer's disease
• Cancer research