Month: October 2022

Yang, Xuefeng; Cai, Shuang; Shu, Yue; Deng, Xun; Zhang, Yuanwei; He, Nian; Wan, Lei; Chen, Xu; Qu, Yan; Yu, Shouyang published the artcile< Exosomal miR-487a derived from m2 macrophage promotes the progression of gastric cancer>, Formula: C30H30Cl2N6O2, the main research area is exosomal microRNA macrophage gastric cancer; M2 macrophage; exosome; gastric cancer; microRNA; proliferation; tumorigenesis.

Tumor-associated macrophages contribute to cell growth, development, and metastasis in various cancers. However, the underlying mechanisms of M2 macrophage that modulate the progression of gastric cancer (GC) remain largely unknown. In this study, we detected the ratio of macrophages in GC tissues and found that the proportion of M2 macrophages was increased in GC tissues. We then co-cultured GC cells with M1 and M2 macrophages, resp., and then assessed cell proliferation and tumorigenicity of GC cells by MTT and colony formation assay. The results indicated that M2 macrophages promoted the proliferation of GC cells, but M1 not. Besides, GW4869, an exosomes inhibitor, reduced the effects induced by M2 macrophage. Then, we isolated and identified exosomes derived from M1 and M2 macrophage, and confirmed that the exosomes could be taken up by GC cells. We demonstrated that M2 macrophage-exosomes could induce the proliferation and tumorigenesis in vitro and in vivo. Moreover, miR-487a was enriched in M2 macrophage-exosomes and further determined that miR-487a exert the functions by targeting TIA1. In conclusion, exosomal miR-487a derived from M2 macrophage promotes the proliferation and tumorigenesis in gastric cancer, and the novel findings might be helpful to the development of novel diagnostic and therapeutic methods in GC.

Cell Cycle published new progress about Animal gene, Slc11a1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (bcg-823). 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Formula: C30H30Cl2N6O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Konishi, Hideyuki; Muto, Takashi; Ueda, Tsuyoshi; Yamada, Yayoi; Yamaguchi, Miyuki; Manabe, Kei published the artcile< Imidazole Derivatives as Accelerators for Ruthenium-Catalyzed Hydroesterification and Hydrocarbamoylation of Alkenes: Extensive Ligand Screening and Mechanistic Study>, Recommanded Product: 2-(tert-Butyl)-1H-imidazole, the main research area is imidazole derivative accelerator ruthenium catalyzed hydroesterification hydrocarbamoylation alkene mechanism.

Imidazole derivatives are effective ligands for promoting the [Ru3(CO)12]-catalyzed hydroesterification of alkenes using formates. Extensive ligand screening was performed to identify 2-hydroxymethylated imidazole as the optimal ligand. Neither carbon monoxide gas nor a directing group was required, and the reaction also showed a wide substrate generality. The Ru-imidazole catalyst system also promoted intramol. hydrocarbamoylation to afford lactams. A Ru-imidazole complex was unambiguously analyzed by x-ray crystallog., and it had a trinuclear structure derived from one [Ru3(CO)12] and two ligands. This complex was also successfully used for hydroesterification. The mechanism was examined in detail by using D- and 13C-labeled formates, indicating that the hydroesterification reaction proceeds by a decarbonylation-recarbonylation pathway.

ChemCatChem published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 36947-69-0 belongs to class imidazoles-derivatives, and the molecular formula is C7H12N2, Recommanded Product: 2-(tert-Butyl)-1H-imidazole.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Gibson, Christoph; Schnatbaum, Karsten; Pfeifer, Jochen R.; Locardi, Elsa; Paschke, Matthias; Reimer, Ulf; Richter, Uwe; Scharn, Dirk; Faussner, Alexander; Tradler, Thomas published the artcile< Novel Small Molecule Bradykinin B2 Receptor Antagonists>, Reference of 1003-21-0, the main research area is small mol bradykinin B2 receptor antagonist preparation structure.

Blockade of the bradykinin B2 receptor provides therapeutic benefit in hereditary angioedema (HAE) and potentially in many other diseases. Herein, we describe the development of highly potent B2 receptor antagonists with a mol. weight of approx. 500 g/mol. First, known quinoline-based B2 receptor antagonists were stripped down to their shared core motif 53, which turned out to be the min. pharmacophore. Targeted modifications of 53 resulted in the highly water-soluble lead compound 8a. Extensive exploration of its structure-activity relationship resulted in a series of highly potent B2 receptor antagonists, featuring a hydrogen bond accepting functionality, which presumably interacts with the side chain of Asn-107 of the B2 receptor. Optimization of the microsomal stability and cytochrome P 450 inhibition eventually led to the discovery of the highly potent and orally available B2 receptor antagonist 52e (JSM10292), which showed the best overall properties.

Journal of Medicinal Chemistry published new progress about Angioedema. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Reference of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Wu, Bingrui; Sun, Dalong; Ma, Lijie; Deng, Yiran; Zhang, Si; Dong, Ling; Chen, She published the artcile< Exosomes isolated from CAPS1-overexpressing colorectal cancer cells promote cell migration>, Product Details of C30H30Cl2N6O2, the main research area is CAPS1 exosome cell migration colorectal cancer.

Calcium-dependent activator protein for secretion 1 (CAPS1) has been reported to promote metastasis in colorectal cancer (CRC), however, the underlying mechanisms have not yet been elucidated. The present study revealed that exosomes derived from CAPS1-overexpressing CRC cells could enhance the migration of normal colonic epithelial FHC cells. GW4869, an inhibitor of exosomes, could attenuate the migration of FHC cells. Furthermore, liquid chromatog.-mass spectrometry (LC-MS) and bioinformatics anal. demonstrated that overexpression of CAPS1 could alter the expression pattern of exosomal proteins involved in cell migration. Bone morphogenetic protein 4, which may serve vital roles in the process of CAPS1-induced cell migration, was downregulated in the exosomes. In summary, the present results demonstrated that CAPS1 promotes cell migration by regulating exosomes. Inhibiting the secretion of exosomes may be helpful for the treatment of patients with metastatic CRC.

Oncology Reports published new progress about Bone morphogenetic protein 4 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Product Details of C30H30Cl2N6O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Fonseca, E.; Demetrio da Silva, V.; Klitzke, J. S.; Schrekker, H. S.; Amico, S. C. published the artcile< Imidazolium ionic liquids as fracture toughening agents in DGEBA-TETA epoxy resin>, Formula: C6H9ClN2O2, the main research area is epoxy resin imidazolium ionic liquid mech thermal property.

Although epoxy resins are used in a broad variety of applications due to their good mech. and thermal properties, their low fracture toughness is a limitation, exhibiting brittle behavior. This study explored the potential use of imidazolium ionic liquids (IL) as toughening agents for epoxy resin based on diglycidyl ether of bisphenol A (DGEBA) with triethylenetetramine (TETA) as curing agent. Fracture toughness was evaluated for DGEBA-TETA epoxy resins with eleven imidazolium IL and the best results were found for the IL with the chloride anion and the shortest N-alkyl side chain, C4MImCl. The use of 1.0 phr of C4MImCl lead to the reduction of the crosslink d. of the post-cured resin, resulting in the increase of 25.5% in stress intensity factor and 8.2% in tensile strength with no significant loss in other mech. properties.

Polymer Testing published new progress about Bending strength. 700370-07-6 belongs to class imidazoles-derivatives, and the molecular formula is C6H9ClN2O2, Formula: C6H9ClN2O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Zhu, Mei; Dong, Biao; Zhang, Guo-Ning; Wang, Ju-Xian; Cen, Shan; Wang, Yu-Cheng published the artcile< Synthesis and biological evaluation of new HIV-1 protease inhibitors with purine bases as P2-ligands>, Reference of 452-06-2, the main research area is HIV1 protease inhibitor purine base derivative; Biological evaluation; HIV-1 protease inhibitors; Purine bases.

Introducing purine bases to P2-ligands might enhance the potency of Human Immunodeficiency Virus-1 (HIV-1) protease inhibitory because of the carbonyl and NH groups promoting the formation of extensive H-bonding interactions. In this work, thirty-three compounds are synthesized and evaluated, among which inhibitors 16a, 16f and 16j (I – III, resp.) containing N-2-(6-substituted-9H-purin-9-yl)acetamide as the P2-ligands along with 4-methoxylphenylsulfonamide as the P2′-ligand, display potent inhibitory effect on the activity of HIV-1 protease with IC50 43 nM, 42 nM and 68 nM in vitro, resp.

Bioorganic & Medicinal Chemistry Letters published new progress about AIDS (disease). 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Reference of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Zhu, Zhensen; Chen, Bo; Peng, Liang; Gao, Songying; Guo, Jingdong; Zhu, Xiongxiang published the artcile< Blockade of LINC01605-enriched exosome generation in M2 macrophages impairs M2 macrophage-induced proliferation, migration, and invasion of human dermal fibroblasts>, Safety of p-Benzenediacrylanilide, 4′,4′′-di-2-imidazolin-2-yl-, dihydrochloride, the main research area is dermal fibroblast macrophage proliferation migration invasion LINC01605 exosome; AKT1; LINC01605; exosomes derived from M2 macrophages; hypertrophic scar; miR-493-3p.

Activated M2 macrophages are involved in hypertrophic scar (HS) formation via manipulating the differentiation of fibroblasts to myofibroblasts having the proliferative capacity and biol. function. However, the function of exosomes derived from M2 macrophages in HS formation is unclear. Thus, this study aims to investigate the role of exosomes derived by M2 in the formation of HS. To understand the effect of exosomes derived from M2 macrophages on formation of HS, M2 macrophages were co-cultured with human dermal fibroblast (HDF) cells. Cell Counting Kit-8 assay was performed to evaluate HDF proliferation. To evaluate the migration and invasion of HDFs, wound-healing and transwell invasion assays were performed, resp. To investigate the interaction between LINC01605 and miR-493-3p, a dual-luciferase reporter gene assay was adopted; consequently, an interaction between miR-493-3p and AKT1 was detected. Our results demonstrated that exosomes derived from M2 macrophages promoted the proliferation, migration, and invasion of HDFs. Addnl., we found that long noncoding RNA LINC01605, enriched in exosomes derived from M2 macrophages, promoted fibrosis of HDFs and that GW4869, an inhibitor of exosomes, could revert this effect. Mechanistically, LINC01605 promoted fibrosis of HDFs by directly inhibiting the secretion of miR-493-3p, and miR-493-3p down-regulated the expression of AKT1. Exosomes derived from M2 macrophages promote the proliferation and migration of HDFs by transmitting LINC01605, which may activate the AKT signaling pathway by sponging miR-493-3p. Our results provide a novel approach and basis for further investigation of the function of M2 macrophages in HS formation.

International Journal of Immunopathology and Pharmacology published new progress about Biomarkers. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Safety of p-Benzenediacrylanilide, 4′,4′′-di-2-imidazolin-2-yl-, dihydrochloride.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Salvitti, Chiara; Pepi, Federico; Manago, Marta; Bortolami, Martina; Michenzi, Cinzia; Chiarotto, Isabella; Troiani, Anna; de Petris, Giulia published the artcile< Free N-heterocyclic carbenes from Bronsted acidic ionic liquids: Direct detection by electrospray ionization mass spectrometry>, Related Products of 700370-07-6, the main research area is methyl carboxymethylimidazolium chloride ionic liquid preparation zwitterion.

The occurrence of N-heterocyclic carbenes in imidazolium-based ionic liquids has long been discussed, but no spectroscopic evidence has been reported yet due to their transient nature. The insertion of an ionizable acid group into the cation scaffold of an ionic liquid which acts as a charge tag allows for the direct detection of free carbenes by mass spectrometry. Three different Broensted acidic ionic liquids were synthesized: 1-methyl-3-carboxymethylimidazolium chloride (MAICl), 1-methyl-3-carboxymethylimidazolium acetate (MAIAc) and the corresponding 2-(3-methyl-1H-imidazol-3-ium-1-yl)acetate zwitterion (MAI – H). The speciation of these compounds was then analyzed by electrospray ionization ion-trap mass spectrometry in the neg. ion mode. The C2-H deprotonation of the imidazolium cation leading to the formation of the corresponding carbene is highly affected by the basic properties of the counter-anion. In the case of MAICl and MAI – H ionic liquids, no charged species corresponding to the free N-heterocyclic carbene was detected. On the contrary, in the presence of a sufficiently basic anion, such as acetate of MAIAc ionic liquid, an intense signal related to the free carbenic species was observed without the addition of an external base. In situ formation of free N-heterocyclic carbenes from Broensted acidic ionic liquids was demonstrated, highlighting the crucial role of anion basicity in promoting the C2-H proton abstraction from imidazolium cations with a carboxylic side chain.

Rapid Communications in Mass Spectrometry published new progress about Collision-induced dissociation. 700370-07-6 belongs to class imidazoles-derivatives, and the molecular formula is C6H9ClN2O2, Related Products of 700370-07-6.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Laviron, Etienne published the artcile< Polarographic and physicochemical studies of nitro, halo-, and carbonyl derivatives of imidazol>, Formula: C4H5BrN2, the main research area is .

The equilibrium between 2 forms of imidazole substituted in position 4 or 5 was investigated. In acidic solutions, the E1/2 values of 4-nitroimidazole (I) and 4-nitro-1-methylimidazole as well as their ultraviolet absorption spectra are identical, indicating that the form A of I predominates over B. The difference in E1/2 between I and 2-nitroimidazole is sufficient for analysis of their mixture The last of the 3 polarographic waves of 2,4,5-triiodoimidazole corresponds to the wave of 2-iodoimidazole, the iodine atom in position 2 being most difficultly reducible. The ratio of the concentrations of form A and B of 4-bromoimidazole is equal to the ratio of the ionization constants of 4-bromo-1-methylimidazole and 5-bromo-1-methylimidazole, viz., 35. Imidazole-4-carboxaldehyde in MeOH or EtOH formed a polarographically inactive hemiacetal.

Compt. Rend. published new progress about 1003-21-0. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Formula: C4H5BrN2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Kuznetsova, A. A.; Kladova, O. A.; Barthes, Nicolas P. F.; Michel, Benoit Y.; Burger, Alain; Fedorova, O. S.; Kuznetsov, N. A. published the artcile< Comparative Analysis of Nucleotide Fluorescent Analogs for Registration of DNA Conformational Changes Induced by Interaction with Formamidopyrimidine-DNA Glycosylase Fpg>, SDS of cas: 452-06-2, the main research area is Escherichia DNA Fpg aPu 3HC Cpy tC0.

Abstract: DNA-substrates containing fluorescent DNA base analogs are widely used to study protein-nucleic acid interactions. In the case of DNA-recognizing enzymes, this approach allows one to register conformational changes in DNA during the formation of enzyme-substrate complexes. An important part of such research is the design of model DNA substrates, which includes both the photophys. properties of the fluorescent groups and their location relative to a specific recognition site, namely, in the same chain on the 5′-, 3′-side or in the complementary chain opposite the specific site. In this work, we report a comparative study of the sensitivity of various fluorescent DNA base analogs, such as 2-aminopurine (aPu), pyrrolocytosine (CPy), 1,3-diaza-2-oxophenoxazine (tCO) and 3-hydroxychromone (3HC), to conformational transformations of DNA in the process of interaction with formamidopyrimidine-DNA glycosylase (Fpg) from Escherichia coli.

Russian Journal of Bioorganic Chemistry published new progress about DNA Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, SDS of cas: 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem