Day: October 17, 2022

Komanova, E.; Knoppova, V.; Koman, V.; Malinova, A. published the artcile< Gas chromatography of isothiocyanates and 3-substituted rhodanines>, SDS of cas: 10574-69-3, the main research area is retention time isothiocyanates; gas chromatog rhodanines.

Retention times in the gas chromatog. separation of 3-substituted alkyl- or arylrhodanines were 5.9 min higher than for the corresponding isothiocyanates, indicating a successful separation of a mixture of these compounds by gas-liquid chromatog. For example, the retention time observed for 4-ethoxyphenyl isothiocyanate was 18.03 min while that of 4-(ethoxyphenyl)-3-rhodanine (I) was 24.02 min. A plot of Hammett constants vs. retention times for 4-substituted isothiocyanates and 3-substituted rhodanines was not linear. Electron-releasing substituents shifted their retention times to lower values while electron-withdrawing substituents had the opposite effect.

Journal of Chromatography published new progress about Linear free energy relationship. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, SDS of cas: 10574-69-3.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Inouye, Satoshi; Sahara-Miura, Yuiko; Nakamura, Mitsuhiro; Hosoya, Takamitsu published the artcile< Expression, purification, and characterization of recombinant apoPholasin>, Category: thiazole, the main research area is apoPholasin glutathione transferase coelenterazine reactive oxygen species oxidation; Coelenteramide; Coelenteramine; Dehydrocoelenterazine; Photoproteins; Reactive oxygen.

Pholasin is a reactive oxygen-sensitive photoprotein that consists of an apoprotein (apoPholasin) and an unknown chromophore. The preferred human codon-optimized apoPholasin gene was transiently expressed in mammalian cells and apoPholasin was detected using an anti-recombinant apoPholasin antibody. For the first time, we found that apoPholasin secreted into the culture medium could catalyze the oxidation of coelenterazine (CTZ, a luciferin) to produce continuous luminescence. The fusion protein of apoPholasin and glutathione S-transferase (GST-apoPholasin) was successfully expressed as a soluble form in bacterial cells using the cold induction system. The purified GST-apoPholasin also had luminescence activity with CTZ, showing the bioluminescence emission peak at 461 nm, and the resultant product showed purple blue fluorescence under 365 nm light. Unexpectedly, the main oxidation product of CTZ was identified as coelenteramine (CTM), not coelenteramide (CTMD).

Protein Expression and Purification published new progress about Absorption. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Category: thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Hasgur, Suheyla; Desbourdes, Laura; Relation, Theresa; Overholt, Kathleen M.; Stanek, Joseph R.; Guess, Adam J.; Yu, Minjun; Patel, Pratik; Roback, Linda; Dominici, Massimo; Otsuru, Satoru; Horwitz, Edwin M. published the artcile< Splenic macrophage phagocytosis of intravenously infused mesenchymal stromal cells attenuates tumor localization>, Safety of (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is mesenchymal stromal cell splenic macrophage phagocytosis tumor localization; cancer cell therapy; lentiviral transduction; mesenchymal stromal cells (MSCs); phagocytosis; splenic macrophage; stem cell transplantation; tumor homing.

Mesenchymal stromal cells (MSCs) possess remarkable tumor tropism, making them ideal vehicles to deliver tumor-targeted therapeutic agents; however, their value in clin. medicine has yet to be realized. A barrier to clin. utilization is that only a small fraction of infused MSCs ultimately localize to the tumor. In an effort to overcome this obstacle, we sought to enhance MSC trafficking by focusing on the factors that govern MSC arrival within the tumor microenvironment. Our findings show that MSC chemoattraction is only present in select tumors, including osteosarcoma, and that the chemotactic potency among similar tumors varies substantially. Using an osteosarcoma xenograft model, we show that human MSCs traffic to the tumor within several hours of infusion. After arrival, MSCs are observed to localize in clusters near blood vessels and MSC-associated bioluminescence signal intensity is increased, suggesting that the seeded cells expand after engraftment. However, our studies reveal that a significant portion of MSCs are eliminated en route by splenic macrophage phagocytosis, effectively limiting the number of cells available for tumor engraftment. To increase MSC survival, we transiently depleted macrophages with liposomal clodronate, which resulted in increased tumor localization without substantial reduction in tumor-associated macrophages. Our data suggest that transient macrophage depletion will significantly increase the number of MSCs in the spleen and thus improve MSC localization within a tumor, theor. increasing the ED of an anti-cancer agent. This strategy may subsequently improve the clin. efficacy of MSCs as vehicles for the tumor-directed delivery of therapeutic agents.

Cytotherapy published new progress about Adhesion G protein-coupled receptor E1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Safety of (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Plouvier, Bertrand; Bailly, Christian; Houssin, Raymond; Henichart, Jean Pierre published the artcile< Synthesis of two new thiazole-containing oligopeptides as potential DNA minor groove binding analogs of netropsin>, Application of C7H10N2O2S, the main research area is netrospin thiazole analog DNA binding.

On the basis of previous studies on synthetic models related to the antibiotic agents netropsin and distamycin A, the design and synthesis of two potential DNA minor groove ligands I and II are described. I and II were prepared by liquid-phase peptide synthesis from the key compounds Et 2-amino-5-methylthiazole-4-carboxylate and Et 2-aminothiazole-5-carboxylate, resp.

Heterocycles published new progress about 72054-60-5. 72054-60-5 belongs to class thiazole, and the molecular formula is C7H10N2O2S, Application of C7H10N2O2S.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Hayashi, Kumiko; Miyamoto, Miki G.; Niwa, Shinsuke published the artcile< Effects of dynein inhibitor on the number of motor proteins transporting synaptic cargos>, Application In Synthesis of 2222768-84-3, the main research area is dynein inhibitor motor protein synaptic cargo.

Synaptic cargo transport by kinesin and dynein in hippocampal neurons was investigated by noninvasively measuring the transport force based on nonequilibrium statistical mechanics. Although direct phys. measurements such as force measurement using optical tweezers are difficult in an intracellular environment, the noninvasive estimations enabled enumerating force-producing units (FPUs) carrying a cargo comprising the motor proteins generating force. The number of FPUs served as a barometer for stable and long-distance transport by multiple motors, which was then used to quantify the extent of damage to axonal transport by dynarrestin, a dynein inhibitor. We found that dynarrestin decreased the FPU for retrograde transport more than for anterograde transport. This result indicates the applicability of the noninvasive force measurements. In the future, these measurements may be used to quantify damage to axonal transport resulting from neuronal diseases, including Alzheimer’s, Parkinson’s, and Huntington’s diseases.

Biophysical Journal published new progress about Alzheimer disease. 2222768-84-3 belongs to class thiazole, and the molecular formula is C22H23F2N3O2S, Application In Synthesis of 2222768-84-3.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Sun, Hua; Mu, Zifeng; Yang, Canglei; Zhang, Kai; Ji, Xingyu; Zhang, Tianshu; Ding, Huanda; Wang, Shifan; Dong, Liming; Zhang, Jing; Zhang, Qichun published the artcile< Facile Azabenz-Annulations through UV-induced Photocyclization: A Promising Method for Perylenediimide-Based Organic Semiconductors>, Quality Control of 1003-32-3, the main research area is bis azabenz annulated perylenediimide preparation optical electrochem semiconducting property; azabenz-annulations; perylenediimides; photocyclization; semiconductors; ultraviolet-induced.

Herein, four bis-azabenz-annulated PDIs (bis-AzaBPDIs) I (Ar = Ph, thiophen-2-yl, 2-cyanothiophen-5-yl, thiazol-5-yl) are concisely synthesized in high yields through UV-induced photocyclization, where the reaction processes including aldimine condensation, cyclization, and oxidative re-aromatization are investigated. The optical characterizations and theor. simulation reveal that the unique properties of the four bis-AzaBPDIs are comparable to their parent PDI. Organic field effect transistors with compounds I (Ar = thiophen-2-yl, 2-cyanothiophen-5-yl, thiazol-5-yl) as active layers indicated that all compounds showed unipolar electron transport properties with the mobilities of 1.1×10-3, 5.8×10-4, and 8.5×10-6 cm2 V-1 s-1, resp. These results suggest the great potential of bis-AzaBPDIs as organic semiconductors. The easy preparation approach reported in this work would renew research interest in developing bis-AzaBPDI-based optoelectronic mols.

Chemistry – An Asian Journal published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Quality Control of 1003-32-3.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Takakura, Hideo published the artcile< Molecular design of D-luciferin-based bioluminescence and 1,2-dioxetane-based chemiluminescence substrates for altered output wavelength and detecting various molecules>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is review luciferin bioluminescence chemiluminescence substrate imaging reagent mol design; bioluminescence; chemiluminescence; design strategy; imaging; molecular probes; near infrared.

A review. Optical imaging including fluorescence and luminescence is the most popular method for the in vivo imaging in mice. Luminescence imaging is considered to be superior to fluorescence imaging due to the lack of both autofluorescence and the scattering of excitation light. To date, various luciferin analogs and bioluminescence probes have been developed for deep tissue and mol. imaging. Recently, chemiluminescence probes have been developed based on a 1,2- dioxetane scaffold. In this , the accumulated findings of numerous studies and the design strategies of bioluminescence and chemiluminescence imaging reagents are summarized.

Molecules published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Kadota, Ayano; Moriguchi, Misato; Watanabe, Tadashi; Sekine, Yuichi; Nakamura, Shigeo; Yasuno, Takumi; Ohe, Tomoyuki; Mashino, Tadahiko; Fujimuro, Masahiro published the artcile< A pyridinium-type fullerene derivative suppresses primary effusion lymphoma cell viability via the downregulation of the Wnt signaling pathway through the destabilization of β-catenin>, Product Details of C11H8N2O3S2, the main research area is Wnt beta catenin pyridinium fullerene suppression primary effusion lymphoma; Kaposi’s sarcoma‑associated herpesvirus; Wnt signaling; fullerene; primary effusion lymphoma; pyridinium fullerene; β‑catenin.

Primary effusion lymphoma (PEL) is defined as a rare subtype of non-Hodgkin′s B cell lymphoma, which is caused by Kaposi′s sarcoma-associated herpesvirus (KSHV) in immunosuppressed patients. PEL is an aggressive type of lymphoma and is frequently resistant to conventional chemo- therapeutics. Therefore, the discovery of novel drug candidates for the treatment of PEL is of utmost importance. In order to discover potential novel anti-tumor compounds against PEL, the authors previously developed a pyrrolidinium-type fullerene derivative, 1,1,1′,1′-tetramethyl [60]fullerenodi- pyrrolidinium diiodide (derivative #1), which induced the apoptosis of PEL cells via caspase-9 activation. In the present study, the growth inhibitory effects of pyrrolidinium-type (derivatives #1 and #2), pyridinium-type (derivatives #3 and #5 to #9) and anilinium-type fullerene derivatives (derivative #4) against PEL cells were evaluated. This anal. revealed a pyridinium-type derivative (derivative #5; 3-5′-(ethoxycarbonyl)-1′,5′-dihydro-2′H-[5,6]fullereno-C60-Ih-[1,9-c] pyrrol-2′-yl-1-methylpyridinium iodide), which exhibited antitumor activity against PEL cells via the downregulation of Wnt/β-catenin signaling. Derivative #5 suppressed the viability of KSHV-infected PEL cells compared with KSHV-uninfected B-lymphoma cells. Furthermore, derivative #5 induced the destabilization of β-catenin and suppressed β-catenin-TCF4 transcriptional activity in PEL cells. It is known that the constitutive activation of Wnt/β-catenin signaling is essential for the growth of KSHV-infected cells. The Wnt/β-catenin activation in KSHV-infected cells is mediated by KSHV latency-associated nuclear antigen (LANA). The data demonstrated that derivative #5 increased β-catenin phosphorylation, which resulted in β-catenin polyubiquitination and subsequent degradation Thus, derivative #5 overcame LANA-mediated β-catenin stabilization. Furthermore, the administration of derivative #5 suppressed the development of PEL cells in the ascites of SCID mice with tumor xenografts derived from PEL cells. On the whole, these findings provide evidence that the pyridinium-type fullerene derivative #5 exhibits antitumor activity against PEL cells in vitro and in vivo. Thus, derivative #5 may be utilized as a novel therapeutic agent for the treatment of PEL.

Oncology Reports published new progress about Adenomatous polyposis coli proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Product Details of C11H8N2O3S2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

He, Bai; Velaparthi, Subash; Pieffet, Gilles; Pennington, Chris; Mahesh, Aruna; Holzle, Denise L.; Brunsteiner, Michael; van Breemen, Richard; Blond, Sylvie Y.; Petukhov, Pavel A. published the artcile< Binding Ensemble Profiling with Photoaffinity Labeling (BEProFL) Approach: Mapping the Binding Poses of HDAC8 Inhibitors>, Synthetic Route of 57493-24-0, the main research area is histone deacetylase HDAC8 photoaffinity labeling BEProFL.

A binding ensemble profiling with (f)photoaffinity labeling (BEProFL) approach that utilizes photolabeling of HDAC8 with a probe containing a UV-activated aromatic azide, mapping of the covalent modifications by liquid chromatog.-tandem mass spectrometry, and a computational method to characterize the multiple binding poses of the probe is described. By use of the BEProFL approach, two distinct binding poses of the HDAC8 probe were identified. The data also suggest that an “”upside-down”” pose with the surface binding group of the probe bound in an alternative pocket near the catalytic site may contribute to the binding.

Journal of Medicinal Chemistry published new progress about Enzyme functional sites. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Synthetic Route of 57493-24-0.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Choi, Sunju; Matta, Hittu; Gopalakrishnan, Ramakrishnan; Natarajan, Venkatesh; Gong, Songjie; Jeronimo, Alberto; Kuo, Wei-Ying; Bravo, Bryant; Chaudhary, Preet M. published the artcile< A novel thermostable beetle luciferase based cytotoxicity assay>, SDS of cas: 2591-17-5, the main research area is luciferase thermostability isolation beetle anticancer agent cytotoxicity.

Cytotoxicity assays are essential for the testing and development of novel immunotherapies for the treatment of cancer. We recently described a novel cytotoxicity assay, termed the Matador assay, which was based on marine luciferases and their engineered derivatives In this study, we describe the development of a new cytotoxicity assay termed ‘Matador-Glo assay’ which takes advantage of a thermostable variant of Click Beetle Luciferase (Luc146-1H2). Matador-Glo assay utilizes Luc146-1H2 and D-luciferin as the luciferase-substrate pair for luminescence detection. The assay involves ectopic over-expression of Luc146-1H2 in the cytosol of target cells of interest. Upon damage to the membrane integrity, the Luc146-1H2 is either released from the dead and dying cells or its activity is preferentially measured in dead and dying cells. We demonstrate that this assay is simple, fast, specific, sensitive, cost-efficient, and not labor-intensive. We further demonstrate that the Matador-Glo assay can be combined with the marine luciferase-based Matador assay to develop a dual luciferase assay for cell death detection. Finally, we demonstrate that the Luc146-1H2 expressing target cells can also be used for in vivo bioluminescence imaging applications.

Scientific Reports published new progress about Antitumor agents. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, SDS of cas: 2591-17-5.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica