1258013-38-5

Upstream product

• 610-14-0 2-nitrobenzyl chloride 
• 1344033-90-4 tert-butyl 4-((2-(2-(2-butyl-6-chloropyrimidine-4-carboxamido)phenyl)thiazolo[5,4-b]pyridin-6-yl)methoxy)piperidine-1-carboxylate 
• 89943-02-2 2,5-dimethyl-3-aminopyridine 
• 925438-35-3 6-methyl-2-(2-nitrophenyl)thiazolo[5,4-b]pyridine 
• 149744-27-4 N-(2-chloro-5-methylpyridin-3-yl)-2-nitrobenzamide 
• 1344033-89-1 tert-butyl 4-((2-(2-aminophenyl)thiazolo[5,4-b]pyridin-6-yl)methoxy)piperidine-1-carboxylate 
• 1344033-88-0 tert-butyl 4-((2-(2-nitrophenyl)thiazolo[5,4-b]pyridin-6-yl)methoxy)piperidine-1-carboxylate 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 925438-37-5 6-(bromomethyl)-2-(2-nitrophenyl)thiazolo[5,4-b]pyridine 
• 1344033-87-9 2-butyl-6-chloropyrimidine-4-carbonyl chloride 
• 1344033-86-8 2-butyl-6-hydroxypyrimidine-4-carboxylic acid 
• 40876-98-0 sodium 1,4-diethoxy-1,4-dioxobut-2-en-2-olate 
• 1344033-91-5 tert-butyl 4-((2-(2-(6-(1-(tert-butoxycarbonyl)piperidin-4-ylamino)-2-butylpyrimidine-4-carboxamido)phenyl)thiazolo[5,4-b]pyridin-6-yl)methoxy)piperidine-1-carboxylate 

Relevant academic research and scientific papers

Synthesis and Assay of SIRT1-Activating Compounds

The NAD+-dependent deacetylase SIRT1 plays key roles in numerous cellular processes including DNA repair, gene transcription, cell differentiation, and metabolism. Overexpression of SIRT1 protects against a number of age-related diseases including diabetes, cancer, and Alzheimer's disease. Moreover, overexpression of SIRT1 in the murine brain extends lifespan. A number of small-molecule sirtuin-activating compounds (STACs) that increase SIRT1 activity in vitro and in cells have been developed. While the mechanism for how these compounds act on SIRT1 was once controversial, it is becoming increasingly clear that they directly interact with SIRT1 and enhance its activity through an allosteric mechanism. Here, we present detailed chemical syntheses for four STACs, each from a distinct structural class. Also, we provide a general protocol for purifying active SIRT1 enzyme and outline two complementary enzymatic assays for characterizing the effects of STACs and similar compounds on SIRT1 activity.

SIRTUIN ACTIVATORS AND ACTIVATION ASSAYS

Provided are methods and compositions for detecting a compound that activates a sirtuin deacetylase activity on a fluorescent-free activation substrate in vitro. Further provided are sirtuin modulating compounds of the formulas (I)-(XXI), and related compounds (XXXI), (XXXII), (XXXIII), and (XXXIV), including the fluorescent free-substrate SIRT1 activator compounds of formulas (XL), (XI), (XII), and (XIII).