Category: 25055-82-7

Ziemianowicz, Daniel S.; Sarpe, Vladimir; Schriemer, David C. published the artcile< Quantitative Analysis of Protein Covalent Labeling Mass Spectrometry Data in the Mass Spec Studio>, COA of Formula: C4H8N2O, the main research area is protein covalent labeling mass spectrometry.

Covalent labeling with mass spectrometry (CL-MS) provides a direct measure of the chem. and structural features of proteins with the potential for resolution at the amino-acid level. Unfortunately, most applications of CL-MS are limited to narrowly defined differential analyses, where small numbers of residues are compared between two or more protein states. Extending the utility of high-resolution CL-MS for structure-based applications requires more robust computational routines and the development of methodol. capable of reporting of labeling yield accurately. Here, we provide a substantial improvement in the anal. of CL-MS data with the development of an extended plug-in built within the Mass Spec Studio development framework (MSS-CLEAN). All elements of data anal.-from database search to site-resolved and normalized labeling output-are accommodated, as illustrated through the nonselective labeling of the human kinesin Eg5 with photoconverted 3,3′-azibutan-1-ol. In developing the new features within the CL-MS plug-in, we identified addnl. complexities associated with the application of CL reagents, arising primarily from digestion-induced bias in yield measurements and ambiguities in site localization. A strategy is presented involving the use of redundant site labeling data from overlapping peptides, the imputation of missing data, and a normalization routine to determine relative protection factors. These elements together provide for a robust structural interpretation of CL-MS/MS data while minimizing the over-reporting of labeling site resolution Finally, to minimize bias, we recommend that digestion strategies for the generation of useful overlapping peptides involve the application of complementary enzymes that drive digestion to completion.

Analytical Chemistry (Washington, DC, United States) published new progress about Homo sapiens. 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, COA of Formula: C4H8N2O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Das, Joydip published the artcile< Identification of alcohol-binding site(s) in proteins using diazirine-based photoaffinity labeling and mass spectrometry>, HPLC of Formula: 25055-82-7, the main research area is protein alc binding site diazirine photoaffinity labeling mass spectrometry; alcoholism; azialcohol; diazirine; mass spectrometry; photoaffinity labeling.

Defining mol. targets of alc. and understanding the mol. mechanism of alc. actions are necessary to develop effective therapeutics for alc. use disorder (AUD). Here, we describe a detailed protocol for identifying alc.-binding site(s) in proteins using diazirine-based azialc. as photoaffinity labeling agents. Upon photoirradiation, azialc. photoincorporates into alc.-binding proteins. The stoichiometry and site of azialc. photoincorporation can be determined using high-resolution mass spectrometry. Identification of the alc.-binding residues in protein followed by measuring the biol. significance of these residues in regulating alc. action are important steps in characterizing the mol. targets of alc.

Chemical Biology & Drug Design published new progress about Algorithm (SEQUEST). 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, HPLC of Formula: 25055-82-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Kandala, Divya T.; Del Piano, Alessia; Minati, Luca; Clamer, Massimiliano published the artcile< Targeting Translation Activity at the Ribosome Interface with UV-Active Small Molecules>, SDS of cas: 25055-82-7, the main research area is targeting translation ribosome interface UV small mol.

Puromycin is a well-known antibiotic that is used to study the mechanism of protein synthesis and to monitor ribosome activity due to its incorporation into nascent peptide chains. However, puromycin effects outside the ribosome catalytic core remain unexplored. Here, we developed two analogs (3PB and 3PC) of the 3′-end of tyrosylated-tRNA that can efficiently interact with several proteins associated with ribosomes. We biochem. characterized the binding of these analogs and globally mapped the direct small mol.-proteins interactions in living cells using clickable and photoreactive puromycin-like probes in combination with in-depth mass spectrometry. We identified a list of proteins targeted by the mols. during ribosome activity (e.g. GRP78) and we addressed possible uses of the probes to sense the activity of protein synthesis and to capture associated RNA. By coupling genome-wide RNA sequencing methods with these mols., the characterization of unexplored translational control mechanisms will be feasible.

ACS Omega published new progress about Animal gene, GRP78 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, SDS of cas: 25055-82-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Lim, Bumhee; Lee, Jinah; Kim, Byungjin; Lee, Rang; Park, Jaehyun; Oh, Dong-Chan; Gam, Jongsik; Lee, Jeeyeon published the artcile< Target Identification of a 1,3,4-Oxadiazin-5(6H)-One Anticancer Agent via Photoaffinity Labelling>, Application In Synthesis of 25055-82-7, the main research area is oxadiazinone protein anticancer agent photoaffinity labeling probe.

Rational design and synthetic feasibility are critical factors for the photoaffinity labeling (PAL) approach, which can identify protein targets of bioactive small mols. under native cellular conditions. In this study, we developed photoaffinity labeling probes derived from 1,3,4-oxadiazin-5(6H)-ones (OPALs) for LL-2003, a previously reported potential anticancer agent against IGF-1R and Src. Our photoaffinity labeling strategy enabled successful photo-crosslinking of the probes (OPAL-6 and OPAL-8) with the target proteins in both mammalian cell lysates and live MCF7, A549, HepG2 and HeLa cells in situ. In vitro and in situ labeling demonstrated different patterns and expression levels of the proteome, and the strongest band for Src appeared in the A549 cell line. An in-gel fluorescence scan combined with MS/MS anal. of the IGF-1R overexpressed insect proteome labeled by OPAL-6 and OPAL-8 identified the binding location of the synthesized probes.

Asian Journal of Organic Chemistry published new progress about Antitumor agents. 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, Application In Synthesis of 25055-82-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ibert, Quentin; Cauwel, Madeleine; Glachet, Thomas; Tite, Tony; Le Nahenec-Martel, Patricia; Lohier, Jean-Francois; Renard, Pierre-Yves; Franck, Xavier; Reboul, Vincent; Sabot, Cyrille published the artcile< One-Pot Synthesis of Diazirines and 15N2-Diazirines from Ketones, Aldehydes and Derivatives: Development and Mechanistic Insight>, COA of Formula: C4H8N2O, the main research area is ketone aldehyde imine ammonia butyl hypochlorite phenyliodine diacetate cyclization; diazirine one pot preparation.

Broad scope one-pot diazirine synthesis strategies have been developed using two different oxidants depending on the nature of the starting material. In all cases, an inexpensive com. solution of ammonia (NH3) in methanol (MeOH) was employed, avoiding the difficult use of liquid ammonia. With aliphatic ketones, t-Bu hypochlorite (t-BuOCl) was found to be the best oxidant whereas it is preferable to use phenyliodine diacetate (PIDA) with aromatic ketones, aldehydes and imines. The nature of the imine-protecting group is essential and only t-Bu imine allowed the synthesis of 15N2-diazirine with complete 15N incorporation, emphasizing a key trans-imination step in the reaction mechanism. These methods are operationally simple, and tolerant to most functional groups, providing diazirines with yields ranging from 20 to 99%.

Advanced Synthesis & Catalysis published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, COA of Formula: C4H8N2O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Martin-Acosta, Pedro; Meng, Qianli; Klimek, John; Reddy, Ashok P.; David, Larry; Petrie, Stefanie Kaech; Li, Bingbing X.; Xiao, Xiangshu published the artcile< A clickable photoaffinity probe of betulinic acid identifies tropomyosin as a target>, Recommanded Product: 2-(3-Methyl-3H-diazirin-3-yl)ethanol, the main research area is clickable photoaffinity probe betulinic acid tropomyosin; Betulinic acid; Cancer; Diazirine; Natural product; Photoaffinity probe; Tropomyosin.

Target identification of bioactive compounds is important for understanding their mechanisms of action and provides critical insights into their therapeutic utility. While it remains a challenge, unbiased chemoproteomics strategy using clickable photoaffinity probes is a useful and validated approach for target identification. One major limitation of this approach is the efficient synthesis of appropriately substituted clickable photoaffinity probes. Herein, we describe an efficient and consistent method to prepare such probes. We further employed this method to prepare a highly stereo-congested probe based on naturally occurring triterpenoid betulinic acid. With this photoaffinity probe, we identified tropomyosin as a novel target for betulinic acid that can account for the unique biol. phenotype on cellular cytoskeleton induced by betulinic acid.

Acta Pharmaceutica Sinica B published new progress about Bioactive agents. 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, Recommanded Product: 2-(3-Methyl-3H-diazirin-3-yl)ethanol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Lam, Albert T.; Zhang, Xiao-Nan; Courouble, Valentine V.; Strutzenberg, Timothy S.; Pei, Hua; Stiles, Bangyan L.; Louie, Stan G.; Griffin, Patrick R.; Zhang, Yong published the artcile< A Bifunctional NAD+ for Profiling Poly-ADP-Ribosylation-Dependent Interacting Proteins>, Recommanded Product: 2-(3-Methyl-3H-diazirin-3-yl)ethanol, the main research area is poly ADP ribosylation bifunctional fluorescent ligand protein interaction.

Protein poly-ADP-ribosylation (PARylation) is a heterogeneous and dynamic post-translational modification regulated by various writers, readers, and erasers. It participates in a variety of biol. events and is involved in many human diseases. Currently, tools and technologies have yet to be developed for unambiguously defining readers and erasers of individual PARylated proteins or cognate PARylated proteins for known readers and erasers. Here, we report the generation of a bifunctional NAD (NAD+) characterized by diazirine-modified adenine and clickable ribose. By serving as an excellent substrate for poly-ADP-ribose polymerase 1 (PARP1)-catalyzed PARylation, the generated bifunctional NAD+ enables photo-crosslinking and enrichment of PARylation-dependent interacting proteins for proteomic identification. This bifunctional NAD+ provides an important tool for mapping cellular interaction networks centered on protein PARylation, which are essential for elucidating the roles of PARylation-based signals or activities in physiol. and pathophysiol. processes.

ACS Chemical Biology published new progress about Apoptosis. 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, Recommanded Product: 2-(3-Methyl-3H-diazirin-3-yl)ethanol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Zheng, Qizhen; Pang, Zhengyuan; Liu, Jingwei; Zhou, Yi; Sun, Yang; Yin, Zheng; Lou, Zhiyong published the artcile< Photoaffinity palladium reagents for capture of protein-protein interactions>, HPLC of Formula: 25055-82-7, the main research area is photoaffinity palladium reagent cysteine containing protein interaction.

Protein-protein interactions (PPIs) are indispensable in almost all cellular processes. Probing of complex PPIs provides new insights into the biol. system of interest and paves the way for the development of therapeutics. Herein, the authors report a strategy for the capture of protein-protein interactions using photoaffinity palladium reagents. First, the palladium-mediated reagent site specifically transferred a photoaffinity modified aryl group to the designated cysteine residue. Next, the photoaffinity group was activated by UV radiation to trap the proximal protein residue for the formation of a crosslink. This strategy was used to capture the PYL-ABA-PP2C interaction, which is at the core of the abscisic acid (ABA) signaling pathway. The authors’ results indicated that this palladium-mediated strategy can serve as an alternative for incorporating an increasing number of diverse substrates for protein crosslinking through cysteine modifications and can be explored for use in mapping protein-peptide or protein-protein interaction surfaces and in trapping potential interacting partners.

Organic & Biomolecular Chemistry published new progress about Photocrosslinking. 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, HPLC of Formula: 25055-82-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Walko, Martin; Hewitt, Eric; Radford, Sheena E.; Wilson, Andrew J. published the artcile< Design and synthesis of cysteine-specific labels for photo-crosslinking studies>, Electric Literature of 25055-82-7, the main research area is diazirine photocrosslinking reagent crosslinking mass spectrometry.

Chem. crosslinking mass-spectrometry (XL-MS) represents a powerful methodol. to map ligand/biomacromol. interactions, particularly where conventional methods such as X-ray crystallog., NMR (NMR) spectroscopy or cryo-electron microscopy (EM) are not feasible. In this manuscript, we describe the design and synthesis of two new photo-crosslinking reagents that can be used to specifically label free thiols through either maleimido or methanethiosulfonate groups and facilitate PXL-MS workflows. Both crosslinkers are based on light sensitive diazirines – precursors of highly reactive carbenes which offer addnl. advantages over alternative crosslinking groups such as benzophenones and aryl nitrenes given the controlled rapid and more indiscriminate reactivity.

RSC Advances published new progress about Biomacromolecular compounds Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, Electric Literature of 25055-82-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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