Tag: M.W=200-250

Dong, Yan; Li, Kehuang; Xu, Zhixiang; Ma, Haikuo; Zheng, Jiyue; Hu, Zhilin; He, Sudan; Wu, Yiyuan; Sun, Zhijian; Luo, Lusong; Li, Jiajun; Zhang, Hongjian; Zhang, Xiaohu published the artcile< Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors>, Product Details of C12H18BNO2, the main research area is protein palmitoyltransferase Porcupine antagonist synthesis inhibitor Wnt signaling secretion; Antagonist; Cancer therapy; Porcupine; Scaffold hybridization; Wnt signaling pathway.

The Wnt signaling pathway is a pivotal developmental pathway. It operates through control of cellular functions such as proliferation, differentiation, migration and polarity. Aberrant Wnt signaling has been implicated in the formation and metastasis of tumors. Porcupine is a component of the Wnt signaling pathway. It is a member of the membrane-bound O-acyltransferase family of proteins. Porcupine catalyzes the palmitoylation of Wnt proteins, a process which is essential to their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from two known porcupine inhibitor classes. The leading compound 62 demonstrated subnanomolar (IC50 0.11 nM) inhibition of Wnt signaling in a paracrine cellular reporter gene assay. Compound 62 also potently inhibited Wnt secretion into culture medium, an indication of direct inhibition of the porcupine protein. Furthermore, compound 62 showed excellent chem., plasma and liver microsomal stabilities. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors.

Bioorganic & Medicinal Chemistry published new progress about Amide group (in Porcupine antagonists). 660867-80-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H18BNO2, Product Details of C12H18BNO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Tohya, Mari; Watanabe, Shin; Teramoto, Kanae; Uechi, Kohei; Tada, Tatsuya; Kuwahara-Arai, Kyoko; Kinjo, Takeshi; Maeda, Shiro; Nakasone, Isamu; Zaw, Ni Ni; Mya, San; Zan, Khin Nyein; Tin, Htay Htay; Fujita, Jiro; Kirikae, Teruo published the artcile< Pseudomonas asiatica sp. nov., isolated from hospitalized patients in Japan and Myanmar>, Product Details of C6H10O8, the main research area is Pseudomonas 16S rRNA phylogeny; Pseudomonas; human pathogen.

A novel Gram-neg., aerobic, rod-shaped, non-spore-forming bacterial strain, RYU5T, was isolated from a stool sample of an inpatient at a hospital in Okinawa, Japan. The optimal growth temperature of RYU5T was 30°C. Phylogenetic anal. based on the sequences of housekeeping genes, including the 16S rRNA, rpoB, rpoD and gyrB genes, showed that RYU5T was a member of the Pseudomonas putida group and was located close to Pseudomonas monteilii and P. putida. Whole-genome comparisons, using average nucleotide identity and digital DNA-DNA hybridization, confirmed that strain RYU5T should be classified as a novel species of Pseudomonas. Phenotypic characterization tests showed that utilization of d-mannose, d-serine, l-arabinose and d-fructose could distinguish this strain from other related species of the genus Pseudomonas. Based on genetic and phenotypic evidence, strain RYU5T should be classified as a novel species, for which the name Pseudomonas asiatica sp. nov. is proposed. The type strain is RYU5T (= DSM 107182T, = JCM 32716T), with a DNA G + C content of 62.25 mol%.

International Journal of Systematic and Evolutionary Microbiology published new progress about 16S rRNA Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 87-73-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H10O8, Product Details of C6H10O8.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Megias-Sayago, Cristina; Reina, Tomas Ramirez; Ivanova, Svetlana; Odriozola, Jose A. published the artcile< Au/CeO2-ZnO/Al2O3 as versatile catalysts for oxidation reactions: application in gas/liquid environmental processes>, Application In Synthesis of 87-73-0, the main research area is gold cerium zinc aluminum oxide catalyst oxidation reaction; CO oxidation; CeO2-ZnO/Al2O3 catalysts; biomass upgrading; glucose oxidation; gold catalysts.

The present work showcases the versatility of nanogold systems supported on Zn-doped ceria when applied in two important environmental processes, the total CO oxidation, and the liquid phase oxidation of glucose to gluconic acid. In the CO oxidation the suitability of these materials is clearly demonstrated achieving full conversions even at sub-ambient conditions. Regarding the glucose oxidation our materials display high conversion values (always over 50%) and very importantly full or almost full selectivity toward gluconic acid-an added value platform chem. in the context of biomass upgrading routes. The key factors controlling the successful performance on both reactions are carefully discussed and compared to previous studies in literature. To our knowledge this is one of the very few works in catalysis by gold combining liquid and gas phase reactions and represents a step forward in the flexible behavior of nano gold catalysts.

Frontiers in Chemistry (Lausanne, Switzerland) published new progress about Biomass. 87-73-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H10O8, Application In Synthesis of 87-73-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Mikami, Satoshi; Kawasaki, Masanori; Ikeda, Shuhei; Negoro, Nobuyuki; Nakamura, Shinji; Nomura, Izumi; Ashizawa, Tomoko; Kokubo, Hironori; Hoffman, Isaac Dylan; Zou, Hua; Oki, Hideyuki; Uchiyama, Noriko; Hiura, Yuuto; Miyamoto, Maki; Itou, Yuuki; Nakashima, Masato; Iwashita, Hiroki; Taniguchi, Takahiko published the artcile< Discovery of a novel series of pyrazolo[1,5-a]pyrimidine-based phosphodiesterase 2A inhibitors structurally different from N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915), for the treatment of cognitive disorders>, Electric Literature of 660867-80-1, the main research area is pyrazolopyrimidine preparation phosphodiesterase inhibitor SAR; intramolecular hydrogen bond; phospodiesterase 2A; phototoxicity; pyrazolo[1,5-a]pyrimidine; schizophrenia; structure-based drug design.

This article described a drug design strategy for a new series of lead compounds structurally distinct from the clin. candidate TAK-915, and subsequent medicinal chem. efforts to optimize potency, selectivity over other PDE families, and other preclin. properties including in-vitro phototoxicity and in-vivo rat plasma clearance. These efforts resulted in the discovery of N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-6-methyl-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide, which robustly increased 3′,5′-cyclic guanosine monophosphate (cGMP) levels in the rat brain following an oral dose, and moreover, attenuated MK-801-induced episodic memory deficits in a passive avoidance task in rats. These data provide further support to the potential therapeutic utility of PDE2A inhibitors in enhancing cognitive performance.

Chemical & Pharmaceutical Bulletin published new progress about Bioavailability. 660867-80-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H18BNO2, Electric Literature of 660867-80-1.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Polonca, Stefanic published the artcile< Environment Shapes the Intra-species Diversity of Bacillus subtilis Isolates>, COA of Formula: C6H10O8, the main research area is bacillus genetic relatedness diversity environmental selection pressure evolution; Bacillus; Biofilm morphology; Biolog; Diversity; Soil microscale.

Cosmopolitan bacteria are those that are found practically everywhere in the world. One of them is Bacillus subtilis, which can travel around the world through dust storms rising from various deserts. Upon landing, bacterial survival is determined by the ability to adjust to the heterogonous environments and bacteria isolated from extremely different environments, such as desert and riverbank soil, are expected to be less related due to the environmental pressure of each region. However, little is known about the influence of soil and habitat on B. subtilis evolution. Here, we show that desert and riverbank B. subtilis strains differ in genetic relatedness and physiol. traits, such as biofilm morphol. and utilization of carbon sources. Desert strains showed more diversity at the genetic level and were able to utilize more carbon sources than riverbank strains which were highly genetically conserved. Biofilm morphologies of desert and riverbank strains generally segregated and both groups formed different morphol. clusters despite the astonishing diversity observed among riverbank strains. We also show that relatedness of B. subtilis strains does not decrease with distance inside the same habitat, which, together with diversity data implies that the difference in environmental selection pressures plays a fundamental role in the evolution of this species.

Microbial Ecology published new progress about Air. 87-73-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H10O8, COA of Formula: C6H10O8.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ozturk, Yasin; Gunaydin, Caner; Yalcin, Fatma; Naziroglu, Mustafa; Braidy, Nady published the artcile< Resveratrol enhances apoptotic and oxidant effects of paclitaxel through TRPM2 channel activation in DBTRG glioblastoma cells>, Application of C14H12O3, the main research area is .

Numerous studies have reported a strong association between increased production of reactive oxygen species (ROS) and the pathobiol. of several diseases, and cancer in particular. Therefore, manipulation of cellular oxidative stress levels represents an important therapeutic target. Recently, resveratrol (RESV), a naturally occurring phytochem., has been shown to sensitize several cell lines to the anticancer effects of other chemotherapeutic agents, including paclitaxel (PAX). However, the mol. mechanisms of action of RESV through oxidative sensitive TRPM2 channel activation remain unclear. The aim of this study was to evaluate the effect of combination therapy of RESV and PAX on activation of TRPM2 in DBTRG glioblastoma cells. DBTRG cells were divided into four treatment groups: control, RESV (50 μM), PAX (50 μM), and PAX + RESV for 24 h. Our data shows that markers for apoptosis, mitochondrial membrane depolarization and mitochondrial function, intracellular steady-state ROS levels, caspase 3 activity, TRPM2 c.d., and Ca2+ florescence intensity were significantly increased in DBTRG cells following treatment with PAX and RESV, resp., although cell viability was also decreased by these treatments. These biochem. markers were further increased to favor the anticancer effects of PAX in DBTRG cells in combination with RESV. The PAX and RESV-mediated increase in c.d. and Ca2+ florescence intensity was decreased with a TRPM2 blocker. This suggests that for this combination therapy to have a substantial effect on apoptosis and cell viability, the TRPM2 channel must be stimulated.

Oxidative Medicine and Cellular Longevity published new progress about 501-36-0 . 501-36-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H12O3, Application of C14H12O3.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Yuan, Li; Zhou, Mengmeng; Huang, Dawei; Wasan, Harpreet S; Zhang, Kai; Sun, Leitao; Huang, Hong; Ma, Shenglin; Shen, Minhe; Ruan, Shanming published the artcile< Resveratrol inhibits the invasion and metastasis of colon cancer through reversal of epithelial‑ mesenchymal transition via the AKT/GSK‑3β/Snail signaling pathway.>, Quality Control of 501-36-0 , the main research area is .

The identification of safe and effective drugs that inhibit tumor invasion and metastasis is required to improve the clinical outcome of patients with colon cancer. The present study aimed to investigate the inhibitory effects and possible mechanisms of action of resveratrol against the invasion and metastasis of colon cancer. AKT1‑knockdown SW480 and SW620 colon cancer cells were used to detect the effects of resveratrol on cell invasion and metastasis, as well as changes in the expression of epithelial‑mesenchymal transition (EMT) markers and serine/threonine kinase (AKT)/glycogen synthase kinase (GSK)‑3β/Snail signaling pathway‑related molecules in vitro. Furthermore, nude mice were inoculated with SW480 cells in the tail vein to establish an in vivo lung metastasis model of colon cancer, to investigate the effects of resveratrol on lung metastasis in colon cancer. The results revealed that resveratrol treatment and AKT1 knockdown significantly inhibited cell migration and invasion in colon cancer, and markedly increased E‑cadherin expression and decreased that of N‑cadherin, phospho (p)‑AKT1, p‑GSK‑3β, and Snail in colon cancer both in vitro and in vivo. Furthermore, the effects of resveratrol were significantly weaker in the AKT1‑knockdown cells. In conclusion, resveratrol may suppress the invasion and metastasis of colon cancer through reversal of EMT via the AKT/GSK‑3β/Snail signaling pathway. AKT1 may therefore be a key regulator of EMT in colon cancer cells and a potential therapeutic target for this disease.

Molecular medicine reports published new progress about 501-36-0 . 501-36-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H12O3, Quality Control of 501-36-0 .

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Hazra, Anindita; Das, Susmita published the artcile< Comparative metabolomics analysis and radical scavenging activity of Saraca asoca (Roxb.) de wilde flowers in different stages of maturity>, HPLC of Formula: 87-73-0, the main research area is Saraca flower maturity metabolomics radical scavenging.

The flower extracts of Saraca asoca were evaluated in their three different phenol. stages of flowering [bud (S1), mature (S2) and senescent (S3)] in terms of chem. composition and antioxidant activity. The GC/MS based fingerprinting led to identification of 85 metabolites, including 9 amino acids, 20 organic acids, 7 fatty acids, 20 sugar and sugar acids, 8 sugar alcs., 13 phenols and phenolic acids and 8 others compounds The three flowering stages showed prominent changes in their metabolite profile during the process of maturation of the flowering stages from bud to mature to senescence stages determined via GC/MS based metabolomics and chemometric approaches. The amounts and composition of metabolites in each stage showed statistically significant differences, which were reflected in their antioxidant capacities. The three phenol. stages showed antioxidant activities in a dose dependent manner, but the senescent stage showed highest superoxide radical scavenging activity (IC50 = 65.17 ± 2.647 mg/mL) and metal chelating effect (6.65 ± 0.331 mg/mL) in agreement with their high content of phenolic acids. These differences were strongly reproduced in the chemometric analyses (PCA, PLS-DA and s-PLS-DA), identifying the most distinctive features of the three flowering stages. This study might be beneficial to select the most potent flowering stage for incorporation in functional food.

Jordan Journal of Biological Sciences published new progress about Alditols Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 87-73-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H10O8, HPLC of Formula: 87-73-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Soares da Costa, Diana; Sousa, Joao C.; Da Mesquita, Sandro; Petkova-Yankova, Nevena I.; Marques, Fernanda; Reis, Rui L.; Sousa, Nuno; Pashkuleva, Iva published the artcile< Bioorthogonal labeling reveals different expression of glycans in mouse hippocampal neuron cultures during their development>, Related Products of 5505-63-5, the main research area is glycan hippocampus neuron cell maturation glucose metabolism; glycosylation, biorthogonal chemistry, neuronal development, imaging..

The expression of different glycans at the cell surface dictates cell interactions with their environment and other cells, being crucial for the cell fate. The development of the central nervous system is associated with tremendous changes in the cell glycome that is tightly regulated. Herein, we have employed bioorthogonal Cu-free click chem. to image temporal distribution of different glycans in live mouse hippocampal neurons during their maturation in vitro. We show development-dependent glycan patterns with increased fucose and decreased mannose expression at the end of the maturation process. We also demonstrate that this approach is biocompatible and does not affect glycan transport although it relies on an administration of modified glycans. The applicability of this strategy to tissue sections unlocks new opportunities to study the glycan dynamics under more complex physiol. conditions.

Molecules published new progress about Carbohydrate transporters Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 5505-63-5 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H14ClNO5, Related Products of 5505-63-5.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Gabriel, Christopher M.; Lee, Nicholas R.; Bigorne, Florence; Klumphu, Piyatida; Parmentier, Michael; Gallou, Fabrice; Lipshutz, Bruce H. published the artcile< Effects of Co-solvents on Reactions Run under Micellar Catalysis Conditions>, Name: 2-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine, the main research area is cosolvent water micelle organic reaction TPGS750M green E factor.

The impact of varying percentages of an organic solvent added to reactions run in aqueous nanomicelles as the reaction medium was studied. Issues such as rates of reaction, percent conversion, and yield, as well as various practical aspects (e.g., effect on stirring, etc.), are discussed, leading to an operationally simple method for the general improvement of potentially problematic systems across a broad range of reaction types, in particular for reactions run at scale.

Organic Letters published new progress about Amidation. 660867-80-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H18BNO2, Name: 2-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts