941575-71-9

Usage

Uses

Used in Pharmaceutical Industry:
3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione is used as a potent GSK-3 inhibitor for the therapeutic treatment of spinal muscular atrophy. Its ability to inhibit the activity of glycogen synthase kinase 3 (GSK-3) makes it a promising candidate for the development of drugs targeting this enzyme, which plays a crucial role in the progression of spinal muscular atrophy.

Upstream product

• 187804-19-9 2-(benzofuran-3-yl)acetamide 
• 25055-67-8 (5-bromo-1-methyl-1H-indol-3-yl)-oxo-acetic acid ethyl ester 
• 108-95-2 phenol 
• 53074-73-0 2-(2-chloroacetyl)phenol 
• 82156-58-9 benzofuran-3-yl-acetic acid ethyl ester 
• 10075-52-2 5-bromo-1-methyl-H-indole 
• 7169-34-8 3-oxo-2,3-dihydrobenzo[b]furan 
• 10075-50-0 5-bromo-1H-indole 
• 143137-54-6 (5-bromo-1-methyl-1H-indol-3-yl)-oxo-acetyl chloride 

Relevant academic research and scientific papers

3-BENZOFURANYL-4-INDOLYL MALEIMIDES AS POTENT GSK3 INHIBITORS FOR NEUROGENERATIVE DISORDERS

Compounds of formula (I): and pharmaceutically acceptable salts, esters and solvates thereof, where variables are defined in the specification, useful generally as inhibitors of protein kinases and particularly useful for inhibition of GSK-3. Pharmaceutically compositions and medicaments containing a compound of the invention are provided. The invention provides methods of treatment of protein kinase-related disease, disorders or conditions. The invention provides methods of treatment of GSK-3-related diseases, disorders or conditions. More specifically, methods of treatment of bipolar disorder, including mania, schizophrenia, stroke, epilepsy, motor neuron disease, cranial or spinal trauma, neurodegenerative disorders, including multiple sclerosis (MS), Alzheimer's disease, Fragile X syndrome, autism, Huntington's disease, Parkinson's

Structure-based design leads to the identification of lithium mimetics that block mania-like effects in rodents. Possible new GSK-3β therapies for bipolar disorders

More than two million American adults, or approximately one percent of the population 18 years or older, suffer from bipolar disorder. Current treatments include the so-called "mood stabilizers," lithium and valproic acid. Both are relatively dated drugs that are only partially effective and produce various undesirable side effects including weight gain. Based upon continued efforts to understand the molecular target for lithium, it now appears that specific inhibitors of the enzyme glycogen synthase kinase-3β (GSK-3β) may mimic the therapeutic action of mood stabilizers and might therefore allow for the design of improved drugs for treating patients with bipolar disorder as well as certain neurodegenerative disorders. Furthermore, the pro-apoptotic properties of the GSK-3 enzyme suggest the possible use of such inhibitors as neuroprotective agents. In fact, neuroprotection may contribute to the treatment of mood disorders. The present chemistry, modeling, and biology efforts have identified 3-benzofuranyl-4-indolylmaleimides as potent and relatively selective GSK-3β inhibitors. The best ligand in this series (having a Ki value of 4.6 nM against GSK-3β) was studied in a novel mouse model of mania that has recently been validated with several clinically effective mood stabilizers. This study presents the first demonstration of the efficacy of a GSK-3β inhibitor in this mouse model of mania. Selective brain penetrable GSK-3 ligands like those described herein become valuable research tools in better defining the role of this multifaceted kinase in both physiological and pathophysiological events.