Kennedy, Cassandra R.; Goya Grocin, Andrea; Kovacic, Tristan; Singh, Ravi; Ward, Jennifer A.; Shenoy, Avinash R.; Tate, Edward W. published the artcile< A Probe for NLRP3 Inflammasome Inhibitor MCC950 Identifies Carbonic Anhydrase 2 as a Novel Target>, Reference of 25055-82-7, the main research area is photoaffinity probe preparation CA2 target inflammasome inhibitor MCC950 inflammation.
Inhibition of inflammasome and pyroptotic pathways are promising strategies for clin. treatment of autoimmune and inflammatory disorders. MCC950, a potent inhibitor of the NLR-family inflammasome pyrin domain-containing 3 (NLRP3) protein, has shown encouraging results in animal models for a range of conditions; however, until now, no off-targets have been identified. Herein, we report the design, synthesis, and application of a novel photoaffinity alkyne-tagged probe for MCC950 (IMP2070) which shows direct engagement with NLRP3 and inhibition of inflammasome activation in macrophages. Affinity-based chem. proteomics in live macrophages identified several potential off-targets, including carbonic anhydrase 2 (CA2) as a specific target of IMP2070, and independent cellular thermal proteomic profiling revealed stabilization of CA2 by MCC950. MCC950 displayed noncompetitive inhibition of CA2 activity, confirming carbonic anhydrase as an off-target class for this compound These data highlight potential biol. mechanisms through which MCC950 and derivatives may exhibit off-target effects in preclin. or clin. studies.
ACS Chemical Biology published new progress about Anti-inflammatory agents (potential as). 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, Reference of 25055-82-7.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts