14703-69-6Relevant articles and documents
Characterization of a New Electron Donor-Acceptor Dyad in Conventional Solvents and Ionic Liquids
Saladin, Marissa,Rumble, Christopher A.,Wagle, Durgesh V.,Baker, Gary A.,Maroncelli, Mark
, p. 9395 - 9407 (2019)
Ionic liquids are being tested as potential replacements for current electrolytes in energy-related applications. Electron transfer (ET) plays a central role in these applications, making it essential to understand how ET in ionic liquids differs from ET in conventional organic solvents and how these differences affect reaction kinetics. A new intramolecular electron donor-acceptor probe was synthesized by covalently linking the popular photoacceptor coumarin 152 with the donor dimethylaniline to create the dyad "C152-DMA" for potential use in probing dynamical solvent effects in ionic liquids. Molecular dynamics simulations of this dyad show the considerable conformational flexibility of the linker group but over a range of geometries in which the ET rate parameters vary little and should have minimal effect on reaction times >100 ps. Steady-state and time-resolved fluorescence methods show the spectra of C152-DMA to be highly responsive to solvent polarity, with ET rates varying over the range of 108 to 1012 s-1 between nonpolar and high-polarity conventional solvents. The sensitivity to hydrolysis in the presence of acidic impurities limits the dyad's use to ionic liquids of high purity. The results in the few ionic liquids examined here suggest that in addition to solvent polarity, electron transfer in C152-DMA also depends on solvent fluidity or solvation times.
Discovery of a novel and potent inhibitor with differential species-specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis
Bin, Huachao,Cao, Zhixing,Chen, Pei,Jiao, Yan,Li, Linli,Lin, Guifeng,Lin, Wanting,Mu, Bo,Nan, Jinshan,Pan, Shulei,Pan, Zhiling,Wang, Falu,Xia, Anjie,Yang, Shengyong,Yang, Shunhua,Zhang, Shanshan,Zhang, Yun,Zhou, Nenghua
, (2022/02/21)
The NLRP3 inflammasome, which regulated a proinflammatory programmed cell death form termed pyroptosis, is involved in the pathological process of various human diseases, such as multiple sclerosis, type 2 diabetes, and gout. Thus, compounds inhibiting activation of the NLRP3 inflammasome can be promising treatments for these diseases. In this study, we conducted a phenotypic screening against NLRP3-dependent pyroptosis and discovered the hit compound 1, which showed moderate antipyroptotic activity. Chemistry efforts to improve potency of 1 resulted in a novel compound 59 (J114), which exhibited a half-maximal inhibitory concentration (IC50) of 0.077 ± 0.008 μM against cell pyroptosis. Interestingly, unlike all pyroptosis inhibitors currently reported, the activity of J114 showed significant differences in human- and mouse-derived cells. The IC50 of J114-mediated inhibition of IL-1β secretion by human THP-1 macrophages was 0.098 μM, which was nearly 150-fold and 500-fold more potent than that of J774A.1 (14.62 μM) and bone marrow-derived macrophages (BMDMs) (48.98 μM), respectively. Further studies showed that J114 displayed remarkable inhibitory activity against NLRP3- and AIM2-but not NLRC4-dependent activation of caspase-1 and the release of IL-1β in human THP-1 macrophages. Mechanistically, J114 disturbed the interaction of NLRP3 or AIM2 with the adaptor protein ASC and inhibited ASC oligomerization. Overall, our study identified a unique molecule that inhibits NLRP3 and AIM2 inflammasome activation and has species differences, which is worthy of further research to understand the differential regulation of the NLRP3 and AIM2 inflammasomes in humans and mice.
Development of trifunctional probes for glycoproteomic analysis
Tsai, Charng-Sheng,Liu, Po-Yu,Yen, Hsin-Yung,Hsu, Tsui-Ling,Wong, Chi-Huey
supporting information; experimental part, p. 5575 - 5577 (2010/09/18)
A new trifunctional probe, assembled using a cleavable linker, is useful for efficient enrichment and detection of alkynyl sugar-tagged biomolecules. The Royal Society of Chemistry 2010.
