Tag: 200-300

On January 31, 2022, Lin, Xian; Tao, Cheng; Zhang, Ren; Zhang, Miaomiao; Wang, Qingwen; Chen, Jian published an article.Category: esters-buliding-blocks The title of the article was N6-methyladenosine modification of TGM2 mRNA contributes to the inhibitory activity of sarsasapogenin in rheumatoid arthritis fibroblast-like synoviocytes. And the article contained the following:

Developing alternative targets and drugs for rheumatoid arthritis (RA) treatment is currently an urgent issue. The relationship between TGM2 and the abnormal immune microenvironment in synovium tissues, as well as the specific role of TGM2 in RA are yet to be elucidated. Sarsasapogenin (Sar) is a sapogenin extracted from the Chinese medical herb Anemarrhena asphodeloides Bunge. and served as a representative anti-inflammatory drug capable of ameliorating inflammatory responses in several human diseases. However, the therapeutic effect of Sar on RA remains unknown. This investigation aims to elucidate the role of TGM2 in RA and investigate whether Sar is a candidate drug to target TGM2 of fibroblast-like synoviocytes (FLS). Bioinformatics analyses were applied for elucidating the role of N(6)-methyladenine (m6A) RNA methylation in RA and identifying the specific target regulated by m6A methylation in RA-FLS. Methylated RNA immunoprecipitation, CCK8 assay, Edu assay, flow cytometry, RT-qPCR and Western blot were utilized to investigate the function of Sar and TGM2 in RA-FLS. Bioinformatics analyses emphasized the importance of m6A RNA methylation in RA and identified an m6A methylation-mediated gene TGM2. Interestingly, both m6A RNA methylation and TGM2 expression in RA synovium tissues correlated with activated immuno-inflammatory phenotype and associated with clin. characteristics and therapy response of RA patients. TGM2 served as a promoter of RA-FLS proliferation by inducing DNA replication and cell cycle transition and inhibiting apoptosis through activating NF-κB signaling. Intriguingly, Sar could impair m6A methylation of TGM2 mRNA and downregulate TGM2 expression. Downregulated TGM2 contributed to the suppressive role of Sar in DNA replication and the stimulatory role of Sar in cell cycle arrest and apoptosis of RA-FLS. Mech., Sar inhibited the expression of key regulators in DNA replication, cell cycle, and apoptosis by impairing NF-κB signaling, thus abolishing FLS proliferation to ameliorate RA progression. This cross-validated work based on three independent datasets is detailedly delineated using cell lines and clin. samples, recognizing that TGM2 can be an attractive target and Sar might be a novel anti-RA drug. The experimental process involved the reaction of Oxybis(ethane-2,1-diyl) bis(2-methylacrylate)(cas: 2358-84-1).Category: esters-buliding-blocks

The Article related to rheumatoid arthritis human sarsasapogenin synoviocytes, n6-methyladenosine, rheumatoid arthritis, sarsasapogenin, tgm2, Placeholder for records without volume info and other aspects.Category: esters-buliding-blocks

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Qian, Yanzhi; Liu, Fengchao; Zhang, Wenguang; Zheng, Xi; Liao, Shengtao; Lv, Lin; Mei, Zhechuan published an article in 2020, the title of the article was AQP9 suppresses hepatocellular carcinoma cell invasion through inhibition of hypoxia-inducible factor 1α expression under hypoxia.SDS of cas: 2358-84-1 And the article contains the following content:

Background and Aim : Intratumor hypoxia is a hallmark of hepatocellular carcinoma (HCC) and is associated with an aggressive tumor phenotype. Although it has been shown that AQP9 plays an important role in HCC, the relevance between hypoxia and AQP9 is still unknown. Methods : We established in vitro normoxic or hypoxic models to investigate the role of AQP9 in the regulation of hypoxia-inducible factor 1α (HIF-1α) and hypoxia-enhanced invasion of hepatoma cells. Mol. expression was detected using western blot or quant. polymerase chain reaction. Cell invasion ability was determined using Transwell invasion assay. In vivo xenograft experiment was used to detect the role of AQP9 on tumor growth. Results : Our present study revealed a decrease in the expression levels of AQP9 in hypoxic microenvironments. Overexpression of AQP9 led to a decreased expression of HIF-1α; conversely, suppression of AQP9 in HCC cells had an opposite effect. Furthermore, up-regulated AQP9 blocked the hypoxic-enhanced invasion of HCC cells. The overexpression of AQP9 inhibited the growth of tumors and HIF-1α expression in vivo. Conclusions : These data suggest that AQP9 acts as a tumor suppressor in HCC invasion via the regulation of HIF-1α expression in the tumor hypoxic microenvironment. The experimental process involved the reaction of Oxybis(ethane-2,1-diyl) bis(2-methylacrylate)(cas: 2358-84-1).SDS of cas: 2358-84-1

The Article related to aqp9 hepatocellular carcinoma cell invasion hif1alpha hypoxia, aquaporin 9, hif-1α, hepatocellular carcinoma, hypoxia, Placeholder for records without volume info and other aspects.SDS of cas: 2358-84-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Abramov, Alex; Maiti, Binoy; Reiser, Oliver; Diaz Diaz, David published an article in 2021, the title of the article was An air-tolerant polymer gel-immobilized iridium photocatalyst with pumping recyclability properties.Formula: C12H18O5 And the article contains the following content:

A novel methacrylate-based cross-linked polymer gel bearing an iridium photocatalyst showed air tolerance and pumping recyclability features through its tunable swelling and deswelling ability. The photocatalytic activity of the polymer gel was demonstrated through an E-to-Z isomerization reaction and in an azide-alkene [2+3] cycloaddition The experimental process involved the reaction of Oxybis(ethane-2,1-diyl) bis(2-methylacrylate)(cas: 2358-84-1).Formula: C12H18O5

The Article related to methacrylate cross linked polymer gel iridium photocatalyst recyclability, photocatalytic isomerization cycloaddition, Placeholder for records without volume info and other aspects.Formula: C12H18O5

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Zurawska, Katarzyna; Stokowy, Marcin; Kapica, Patryk; Olesiejuk, Monika; Kudelko, Agnieszka; Papaj, Katarzyna; Skonieczna, Magdalena; Szeja, Wieslaw; Walczak, Krzysztof; Kasprzycka, Anna published an article in 2021, the title of the article was Synthesis and Preliminary Anticancer Activity Assessment of N-Glycosides of 2-Amino-1,3,4-thiadiazoles.Reference of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate And the article contains the following content:

The addition of 2-amino-1,3,4-thiadiazole derivatives with parallel iodination of differently protected glycals has been achieved using a double molar excess of mol. iodine under mild conditions. The corresponding thiadiazole derivatives of N-glycosides were obtained in good yields and anomeric selectivity. The usage of iodine as a catalyst makes this method easy, inexpensive, and successfully useable in reactions with sugars. Thiadiazole derivatives were tested in a panel of three tumor cell lines, MCF-7, HCT116, and HeLa. These compounds initiated biol. response in investigated tumor models in a different rate. The MCF-7 is resistant to the tested compounds, and the cytometry assay indicated low increase in cell numbers in the sub- G1 phase. The most sensitive are HCT-116 and HeLa cells. The thiadiazole derivatives have a pro-apoptotic effect on HCT-116 cells. In the case of the HeLa cells, an increase in the number of cells in the sub-G1- phase and the induction of apoptosis was observed The experimental process involved the reaction of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate(cas: 2873-29-2).Reference of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate

The Article related to aminothiadiazole glycoside anticancer activity, 1,3,4-thiadiazole, n-glycosides, glycal, molecular iodine, Placeholder for records without volume info and other aspects.Reference of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Krabill, Aaron D.; Chen, Hao; Hussain, Sajjad; Hewitt, Chad S.; Imhoff, Ryan D.; Muli, Christine S.; Das, Chittaranjan; Galardy, Paul J.; Wendt, Michael K.; Flaherty, Daniel P. published an article in 2021, the title of the article was Optimization and anti-cancer properties of fluoromethylketones as covalent inhibitors for ubiquitin C-terminal hydrolase L1.Category: esters-buliding-blocks And the article contains the following content:

The deubiquitinating enzyme (DUB) UCHL1 is implicated in various disease states including neurodegenerative disease and cancer. However, there is a lack of quality probe mols. to gain a better understanding on UCHL1 biol. To this end a study was carried out to fully characterize and optimize the irreversible covalent UCHL1 inhibitor VAEFMK. Structure-activity relationship studies identified modifications to improve activity vs. the target and a full cellular characterization was carried out for the first time with this scaffold. The studies produced a new inhibitor, 34, with an IC50 value of 7.7 μM against UCHL1 and no observable activity vs. the closest related DUB UCHL3. The mol. was also capable of selectively inhibiting UCHL1 in cells and did not demonstrate any discernible off-target toxicity. Finally, the mol. was used for initial probe studies to assess the role of UCHL1 role in proliferation of myeloma cells and migration behavior in small cell lung cancer cells making 34 a new tool to be used in the biol. evaluation of UCHL1. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Category: esters-buliding-blocks

The Article related to uchl fluoromethylketone covalent inhibitor optimization anticancer property, uchl1 inhibitors, covalent inhibitors, deubiquitinases, fluoromethylketones, Placeholder for records without volume info and other aspects.Category: esters-buliding-blocks

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On March 1, 2021, Cao, Rong-An; Ji, RuiXue; Tabarsa, Mehdi; Zhang, JianQiang; Meng, LingQi; Zhang, ChengTai; Zhang, JiaMiao; Wang, LiDong; Wu, Rui; Wang, ChangYuan; Jin, ChengHao; You, SangGuan published an article.Recommanded Product: 2873-29-2 The title of the article was Purification, characterization and immunostimulatory effects of polysaccharides from Anemarrhena asphodeloides rhizomes. And the article contained the following:

The crude polysaccharide was extracted from A. asphodeloides rhizomes and further purified to produce two fractions F1 (50.0%) and F2 (19.6%). The chem. constitutions of the polysaccharides were neutral sugars (51.4%-89.7%), uronic acids (1.0%-30.2%) and sulfate esters (3.4%-8.1%), with various ratios of monosaccharides including rhamnose (1.4%-6.1%), arabinose (7.1%-21.2%), xylose (0.2%-4.8%), mannose (39.9%-79.0%), glucose (6.0%-11.1%) and galactose (2.6%-22.0%). The mol. properties of the polysaccharides were investigated by the HPSEC-UV-MALLS-RI system, revealing the Mw 130.0 × 103-576.5 × 103 g/moL, Rg 87.6-382.6 nm and SVg 0.3-54.3 cm3/g. The polysaccharides stimulated RAW264.7 cells to produce considerable amounts of NO and up-regulate the expression of TNF-α, IL-1 and COX-2 genes. Polysaccharides exhibited the growth inhibitory effects on cancer cells lines of AGS, MKN-28 and MKN-45, in which F2 fraction exhibited prominent bioactivities. The AGS cells treated with F2 experienced condensed cytoplasm, shrinkage of nucleus and chromatin marginalization with the highest number of cells at early-stage apoptosis reaching 54.6%. The inhibitory effect of F2 polysaccharide on AGS cells was through MAPKs and STAT3 signaling pathways. The backbone of the F2 was mainly linked by (1 → 4)-linked mannopyranosyl and (1 → 3)-linked galactopyranosyl. Taken together, the polysaccharide from A. asphodeloides rhizomes could be utilized as medicinal, pharmacol. and functional food ingredients. The experimental process involved the reaction of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate(cas: 2873-29-2).Recommanded Product: 2873-29-2

The Article related to polysaccharide anemarrhena asphodeloides rhizome immunostimulatory purification characterization, characterization, immunostimulatory, polysaccharides, Placeholder for records without volume info and other aspects.Recommanded Product: 2873-29-2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On September 30, 2020, Azambuja, J. H.; Schuh, R. S.; Michels, L. R.; Iser, I. C.; Beckenkamp, L. R.; Roliano, G. G.; Lenz, G. S.; Scholl, J. N.; Sevigny, J.; Wink, M. R.; Stefani, M. A.; Battastini, A. M. O.; Figueiro, F.; Teixeira, H. F.; Braganhol, E. published an article.HPLC of Formula: 2358-84-1 The title of the article was Blockade of CD73 delays glioblastoma growth by modulating the immune environment. And the article contained the following:

Abstract: Immunotherapy as an approach for cancer treatment is clin. promising. CD73, which is the enzyme that produces extracellular adenosine, favors cancer progression and protects the tumor from immune surveillance. While CD73 has recently been demonstrated to be a potential target for glioma treatment, its role in regulating the inflammatory tumor microenvironment has not yet been investigated. Thus, this study explores the immunotherapeutic value of the CD73 blockade in glioblastoma. The immuno-therapeutic value of the CD73 blockade was evaluated in vivo in immunocompetent pre-clin. glioblastoma model. As such, glioblastoma-bearing rats were nasally treated for 15 days with a siRNA CD73-loaded cationic-nanoemulsion (NE-siRNA CD73R). Apoptosis was determined by flow cytometry using Annexin-V staining and cell proliferation was analyzed by Ki67 expression by immunohistochem. The treatment selectively decreased CD73 expression in the GB cells as well as in the tumor-associated-macrophages/microglia. This study indicates that CD73 knockdown using a nanotechnol. approach to perform nasal delivery of siRNA-CD73 to CNS can potentially regulate the glioblastoma immune microenvironment and delay tumor growth by inducing apoptosis. The experimental process involved the reaction of Oxybis(ethane-2,1-diyl) bis(2-methylacrylate)(cas: 2358-84-1).HPLC of Formula: 2358-84-1

The Article related to cd73 glioblastoma growth immune environment, ecto-5′-nucleotidase/cd73, glioblastoma, immunotherapy, macrophages, microglia, t regulatory lymphocytes, Placeholder for records without volume info and other aspects.HPLC of Formula: 2358-84-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On July 5, 2021, Romero, Eugenie; Oueslati, Saoussen; Benchekroun, Mohamed; D′Hollander, Agathe C. A.; Ventre, Sandrine; Vijayakumar, Kamsana; Minard, Corinne; Exilie, Cynthia; Tlili, Linda; Retailleau, Pascal; Zavala, Agustin; Elisee, Eddy; Selwa, Edithe; Nguyen, Laetitia A.; Pruvost, Alain; Naas, Thierry; Iorga, Bogdan I.; Dodd, Robert H.; Cariou, Kevin published an article.Related Products of 141940-37-6 The title of the article was Azetidinimines as a novel series of non-covalent broad-spectrum inhibitors of β-lactamases with submicromolar activities against carbapenemases KPC-2 (class A), NDM-1 (class B) and OXA-48 (class D). And the article contained the following:

The occurrence of resistances in Gram neg. bacteria is steadily increasing to reach extremely worrying levels and one of the main causes of resistance is the massive spread of very efficient β-lactamases which render most β-lactam antibiotics useless. Herein, we report the development of a series of imino-analogs of β-lactams (namely azetidinimines) as efficient non-covalent inhibitors of β-lactamases. Despite the structural and mechanistic differences between serine-β-lactamases KPC-2 and OXA-48 and metallo-β-lactamase NDM-1, all three enzymes can be inhibited at a submicromolar level by compound 7dfm (I), which can also repotentiate imipenem against a resistant strain of Escherichia coli expressing NDM-1. We show that 7dfm can efficiently inhibit not only the three main clin.-relevant carbapenemases of Ambler classes A (KPC-2), B (NDM-1) and D (OXA-48) with Ki′s below 0.3 μM, but also the cephalosporinase CMY-2 (class C, 86% inhibition at 10 μM). Our results pave the way for the development of a new structurally original family of non-covalent broad-spectrum inhibitors of β-lactamases. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Related Products of 141940-37-6

The Article related to azetidinimine noncovalent beta lactamase inhibitor, azetidinimines, bacterial resistance, carbapenemase inhibitors, kpc-2, ndm-1, oxa-48, ynamides, Placeholder for records without volume info and other aspects.Related Products of 141940-37-6

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On June 30, 2006, Balakrishnan, Anand; Wring, Stephen A.; Coop, Andrew; Polli, James E. published an article.HPLC of Formula: 53838-27-0 The title of the article was Influence of Charge and Steric Bulk in the C-24 Region on the Interaction of Bile Acids with Human Apical Sodium-Dependent Bile Acid Transporter. And the article contained the following:

The human apical sodium-dependent bile acid transporter (hASBT) is a potential target for drug delivery, but an understanding of hASBT substrate requirements is limited. The objective of this study was to evaluate the influence of ionic character and steric bulk in the C-24 region of bile acid conjugates in governing interaction with hASBT. Ionic character was studied using chenodeoxycholate (CDCA) conjugates of glutamic acid and lysine, which varied in charge (mono-anionic, di-anionic, cationic, neutral, and zwitterionic) and location of charge (proximal or distal to C-24). Steric effects were evaluated using ester conjugates that varied in ester substituent size (Me, benzyl, and tert-butyl) and location (proximal and/or distal). Conjugate interaction with hASBT was assessed via transport and inhibition studies, using a hASBT-MDCK monolayer. Mono-anionic, cationic, and neutral conjugates of CDCA exhibited high inhibitory potency (Ki < 10 μM). High inhibition potency of neutral and cationic conjugates indicated that a neg. charge is not essential for hASBT binding. Di-anionic conjugates exhibited low inhibition potency (Ki > 100 μM). Conjugates with a single bulky ester substituent proximal or distal to the C-24 region exhibited high inhibition potency. However, two bulky substituents practically abolished interaction. In transport studies, mono-anionic conjugates were high affinity hASBT substrates. Meanwhile, cationic and zwitterionic conjugates were not substrates for hASBT. Overall, C-24 ionic character influenced interaction with hASBT. Although the presence of a single neg. charge was not essential for interaction with hASBT, mono-anionic conjugates were favored for hASBT-mediated transport compared to cationic and zwitterionic conjugates. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).HPLC of Formula: 53838-27-0

The Article related to apical sodium dependent bile acid transporter electrostatic steric effect, asbt protein transport bile acid conjugate electrostatic steric effect, General Biochemistry: Subcellular Processes and other aspects.HPLC of Formula: 53838-27-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On December 31, 2020, Mirzaei, Mehdi; Gupta, Vivek K.; Chitranshi, Nitin; Deng, Liting; Pushpitha, Kanishka; Abbasi, Mojdeh; Chick, Joel M.; Rajput, Rashi; Wu, Yunqi; McKay, Matthew J.; Salekdeh, Ghasem H.; Gupta, Veer B.; Haynes, Paul A.; Graham, Stuart L. published an article.Name: Oxybis(ethane-2,1-diyl) bis(2-methylacrylate) The title of the article was Retinal proteomics of experimental glaucoma model reveal intraocular pressure-induced mediators of neurodegenerative changes. And the article contained the following:

Current evidence suggests that exposure to chronically induced intraocular pressure (IOP) leads to neurodegenerative changes in the inner retina. This study aimed to determine retinal proteomic alterations in a rat model of glaucoma and compared findings with human retinal proteomics changes in glaucoma reported previously. We developed an exptl. glaucoma rat model by subjecting the rats to increased IOP (9.3 ± 0.1 vs 20.8 ± 1.6 mm Hg) by weekly microbead injections into the eye (8 wk). The retinal tissues were harvested from control and glaucomatous eyes and protein expression changes analyzed using a multiplexed quant. proteomics approach (TMT-MS3). Immunofluorescence was performed for selected protein markers for data validation. Our study identified 4304 proteins in the rat retinas. Out of these, 139 proteins were downregulated (≤0.83) while the expression of 109 proteins was upregulated (≥1.2-fold change) under glaucoma conditions (P ≤ .05). Computational anal. revealed reduced expression of proteins associated with glutathione metabolism, mitochondrial dysfunction/oxidative phosphorylation, cytoskeleton, and actin filament organization, along with increased expression of proteins in coagulation cascade, apoptosis, oxidative stress, and RNA processing. The experimental process involved the reaction of Oxybis(ethane-2,1-diyl) bis(2-methylacrylate)(cas: 2358-84-1).Name: Oxybis(ethane-2,1-diyl) bis(2-methylacrylate)

The Article related to glaucomatous retina glycoprotein oxidative stress glaucoma pathogenesis intraocular pressure, glaucoma, neurodegeneration, proteomics, retina, Placeholder for records without volume info and other aspects.Name: Oxybis(ethane-2,1-diyl) bis(2-methylacrylate)

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics