338391-69-8

Upstream product

• 320422-34-2 5-amino-1-tert-butyl-3-(4-fluoro-phenyl)-1H-pyrazole-4-carbonitrile 
• 77287-34-4 formamide 
• 403-43-0 4-fluorobenzoyl chloride 
• 954221-24-0 [(4-fluorophenyl)(methoxy)methylidene]propanedinitrile 
• 956025-35-7 (4-fluorobenzoyl)propanedinitrile 
• 862728-60-7 1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine 
• 158001-28-6 5-amino-1-(tert-butyl)-1H-pyrazole-4-carbonitrile 
• 862728-61-8 3-bromo-1-(tert-butyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine 
• 1765-93-1 4-fluoroboronic acid 

Relevant academic research and scientific papers

Discovery of a potent protein kinase D inhibitor: insights in the binding mode of pyrazolo[3,4-d]pyrimidine analogues

In this study, we set out to rationally optimize PKD inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold. The lead compound for this study was 1-NM-PP1, which was previously found by us and others to inhibit PKD. In our screening we identified one compound (3-IN-PP1) displaying a 10-fold increase in potency over 1-NM-PP1, opening new possibilities for specific protein kinase inhibitors for kinases that show sensitivity towards pyrazolo[3,4-d]pyrimidine derived compounds. Interestingly the observed SAR was not in complete agreement with the commonly observed binding mode where the pyrazolo[3,4-d]pyrimidine compounds are bound in a similar fashion as PKD's natural ligand ATP. Therefore we suggest an alternate binding mode where the compounds are flipped 180 degrees. This possible alternate binding mode for pyrazolo[3,4-d]pyrimidine based compounds could pave the way for a new class of specific protein kinase inhibitors for kinases sensitive towards pyrazolo[3,4-d]pyrmidines.

MODULATION OF PROTEIN TRAFFICKING

Compounds and compositions are provided for treatment or amelioration of one or more disorders characterized by defects in protein trafficking. A method of treating a disorder characterized by impaired protein trafficking includes administering to a subject or contacting a cell with a compound of Formula I: [formula here] or pharmaceutically acceptable salts or derivatives thereof.

INHIBITION OF ALPHA-SYNUCLEIN TOXICITY

Compounds and compositions are provided for treatment or amelioration of one or more symptoms of α-synuclein toxicity, α-synuclein mediated diseases or diseases in which α-synuclein fibrils are a symptom or cause of the disease.

Inhibitors of MAPK/Erk Kinase

The present invention relates to compounds useful as inhibitors of MEK kinase and methods for the treatment or prevention of cellular proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.