Category: 25055-82-7

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

Ziemianowicz, Daniel S.; MacCallum, Justin L.; Schriemer, David C. published the artcile< Correlation between Labeling Yield and Surface Accessibility in Covalent Labeling Mass Spectrometry>, Synthetic Route of 25055-82-7, the main research area is surface accessibility covalent labeling mass spectrometry.

The functional properties of a protein are strongly influenced by its topog., or the solvent-facing contour map of its surface. Together with crosslinking, covalent labeling mass spectrometry (CL-MS) has the potential to contribute topog. data through the measurement of surface accessibility. However, recent efforts to correlate measures of surface accessibility with labeling yield have been met with mixed success. Most applications of CL-MS involve differential anal. of protein interactions (i.e., footprinting experiments) where such inconsistencies have limited effect. Extending CL-MS into structural anal. requires an improved evaluation of the relation between labeling and surface exposure. The authors applied recently developed diazirine reagents to obtain deep coverage of the large motor domain of Eg5 (a mitotic kinesin), and together with computational methods the authors correlated labeling yields with accessibility data in a number of ways. Correlations can indeed be seen at a local structural level, but these correlations do not extend across the structure. The lack of correlation arises from the influence of protein dynamics and chem. composition on reagent partitioning and, thus, also on labeling yield. The authors’ use of CL-MS data should be considered in light of “”chem. accessibility”” rather than “”solvent accessibility”” and suggest that CL-MS data would be a useful tool in the fundamental study of protein-solute interactions.

Journal of the American Society for Mass Spectrometry published new progress about Kinesin-like protein KIF11 Role: ANT (Analyte), BSU (Biological Study, Unclassified), ANST (Analytical Study), BIOL (Biological Study) (Eg5, ADP-bound). 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, Synthetic Route of 25055-82-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Laengle, D.; Wesseler, F.; Floetgen, D.; Leek, H.; Plowright, A. T.; Schade, D. published the artcile< Unique photoaffinity probes to study TGFβ signaling and receptor fates>, COA of Formula: C4H8N2O, the main research area is dihydropyridine annulated preparation transforming growth factor beta pharmacophore SAR.

A novel synthetic approach is used to prepare a diverse set of “”first-in-class”” dihydropyridine-based TGFβ receptor degraders bearing photoaffinity labels. These probes serve as valuable tools to study TGFβ receptor fates and dynamics – an important challenge in chem. biol.

Chemical Communications (Cambridge, United Kingdom) published new progress about Dihydropyridines Role: DGN (Diagnostic Use), PAC (Pharmacological Activity), PEP (Physical, Engineering or Chemical Process), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), USES (Uses), PROC (Process), RACT (Reactant or Reagent), PREP (Preparation). 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

Ziemianowicz, Daniel S.; MacCallum, Justin L.; Schriemer, David C. published the artcile< Correlation between Labeling Yield and Surface Accessibility in Covalent Labeling Mass Spectrometry>, Synthetic Route of 25055-82-7, the main research area is surface accessibility covalent labeling mass spectrometry.

The functional properties of a protein are strongly influenced by its topog., or the solvent-facing contour map of its surface. Together with crosslinking, covalent labeling mass spectrometry (CL-MS) has the potential to contribute topog. data through the measurement of surface accessibility. However, recent efforts to correlate measures of surface accessibility with labeling yield have been met with mixed success. Most applications of CL-MS involve differential anal. of protein interactions (i.e., footprinting experiments) where such inconsistencies have limited effect. Extending CL-MS into structural anal. requires an improved evaluation of the relation between labeling and surface exposure. The authors applied recently developed diazirine reagents to obtain deep coverage of the large motor domain of Eg5 (a mitotic kinesin), and together with computational methods the authors correlated labeling yields with accessibility data in a number of ways. Correlations can indeed be seen at a local structural level, but these correlations do not extend across the structure. The lack of correlation arises from the influence of protein dynamics and chem. composition on reagent partitioning and, thus, also on labeling yield. The authors’ use of CL-MS data should be considered in light of “”chem. accessibility”” rather than “”solvent accessibility”” and suggest that CL-MS data would be a useful tool in the fundamental study of protein-solute interactions.

Journal of the American Society for Mass Spectrometry published new progress about Kinesin-like protein KIF11 Role: ANT (Analyte), BSU (Biological Study, Unclassified), ANST (Analytical Study), BIOL (Biological Study) (Eg5, ADP-bound). 25055-82-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8N2O, Synthetic Route of 25055-82-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Laengle, D.; Wesseler, F.; Floetgen, D.; Leek, H.; Plowright, A. T.; Schade, D. published the artcile< Unique photoaffinity probes to study TGFβ signaling and receptor fates>, COA of Formula: C4H8N2O, the main research area is dihydropyridine annulated preparation transforming growth factor beta pharmacophore SAR.

A novel synthetic approach is used to prepare a diverse set of “”first-in-class”” dihydropyridine-based TGFβ receptor degraders bearing photoaffinity labels. These probes serve as valuable tools to study TGFβ receptor fates and dynamics – an important challenge in chem. biol.

Chemical Communications (Cambridge, United Kingdom) published new progress about Dihydropyridines Role: DGN (Diagnostic Use), PAC (Pharmacological Activity), PEP (Physical, Engineering or Chemical Process), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), USES (Uses), PROC (Process), RACT (Reactant or Reagent), PREP (Preparation). 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

Synthetic Route of 25055-82-7, Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 25055-82-7, name is 2-(3-Methyl-3H-diazirin-3-yl)ethanol. A new synthetic method of this compound is introduced below.

A solution of 2-(3-methyl-3H-diazirin-3-yl)ethan-i-ol (100 mg, 1.0 mmol) and triethylamine (160 mu, 1.15 mmol) in dichloromethane (5 mL) was cooled in an ice bath. To the cooled solution was added methanesulfonyl chloride (93 mu, 1.2 mmol). The reaction mixture was stirred for 1.5 hours in the ice bath, then saturated ammonium chloride was added and the organic layer was separated. The aqueous layer was extracted once with dichloromethane. The organic layers were combined, dried over sodium sulfate, filtered and then concentrated in vacuo to afford the title compound (178 mg, quantitative yield) which was used without further purification. (1292) NMR (CDC13): delta = 4.13 (t, 2 Eta), 3.05 (s, 3 Eta), 1.79 (t, 2 Eta), 1.09 (s, 3 Eta).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,25055-82-7, its application will become more common.

Reference:
Patent; INFLAZOME LIMITED; COOPER, Matthew; MILLER, David; MACLEOD, Angus; VAN WILTENBURG, Jimmy; THOM, Stephen; ST-GALLAY, Stephen; SHANNON, Jonathan; (352 pag.)WO2019/8025; (2019); A1;,
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Related Products of 25055-82-7, Adding some certain compound to certain chemical reactions, such as: 25055-82-7, name is 2-(3-Methyl-3H-diazirin-3-yl)ethanol,molecular formula is C4H8N2O, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 25055-82-7.

4-hydroxy-2-butanone (20, 1.00 g, 11.35 mmol) was pipetted into a dry flask and cooled to 0C under nitrogen atmosphere. 7N methanolic ammonia (11.2 mL, 79 mmol) was added via syringe, and the solution was allowed to stir at 0C for 3 hours. A solution of hydroxylamine-O-sulfonic acid (1.476 g, 13.05 mmol) in methanol (9.7 mL) was added dropwise, then was allowed to stir for an additional 16 hours while slowly warming to room temperature. The reaction was filtered through a sintered glass funnel, then transferred to a reaction vessel and re-cooled to 0C. Triethylamine (1.58 mL,11.35 mmol) was added, then molecular iodine (2.88 g, 11.35 mmol) was added slowly in 10 equal portions until the purple/brown color of iodine persisted in the reaction vessel. The solvent was removed under reduced pressure, and purification of the crude isolate via Kugelrohr distillation (60C, 1-3 torr) delivered the 2,2-diazirinyl intermediate as a clear oil (304 mg, 27% yield). A portion of this intermediate (300 mg, 3.00 mmol) was dissolved in dry pyridine (6 mL) and cooled to 0C in an ice bath. To this solution was added p-toluenesulfonyl chloride (628 mg, 3.30 mmol). The reaction mixture was allowed to stir for 24 hours at 0-4C, then was poured into a mixture of 37%w/v HCl (15 mL) and ice (80 mL). The resulting suspension was extracted 3x with ether, then the pooled organic layers were washed with 1N HCl solution, 1N NaOH solution, water, and brine. The organic extract was dried over MgSO4, vacuum filtered, and concentrated to a clear oil (428 mg, 15% yield over 3 steps) used without further purification. TLC Rf (2:1 hex:EtOAc) = 0.6. 1HNMR (500 MHz, CDCl3) delta 7.82 (d, J = 7.9 Hz, 2H), 7.37 (d, J= 7.9 Hz, 2H), 3.96 (t, J = 6.4 Hz, 2H), 2.46 (s, 3H), 1.68 (t, J= 6.4 Hz, 2H), 1.01 (s, 2H).

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 25055-82-7, 2-(3-Methyl-3H-diazirin-3-yl)ethanol, other downstream synthetic routes, hurry up and to see.

Reference:
Article; Yestrepsky, Bryan D.; Kretz, Colin A.; Xu, Yuanxi; Holmes, Autumn; Sun, Hongmin; Ginsburg, David; Larsen, Scott D.; Bioorganic and Medicinal Chemistry Letters; vol. 24; 6; (2014); p. 1538 – 1544;,
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts