Tag: M.W=250-300

Yang, Xingye; Qin, Xiaojun; Ji, Huimin; Du, Lupei; Li, Minyong published the artcile< Constructing firefly luciferin bioluminescence probes for in vivo imaging>, Application of C11H8N2O3S2, the main research area is .

Bioluminescence imaging (BLI) is a widely applied visual approach for real-time detecting many physiol. and pathol. processes in a variety of biol. systems. Based on the caging strategy, lots of bioluminescent probes have been well developed. While the targets react with recognizable groups, caged luciferins liberate luciferase substrates, which react with luciferase generating a bioluminescent response. Among the various bioluminescent systems, the most widely utilized bioluminescent system is the firefly luciferin system. The H and carboxylic acid of luciferin are critically caged sites. The introduced self-immolative linker extends the applications of probes. Firefly luciferin system probes have been successfully applied for analyzing physiol. processes, monitoring the environment, diagnosing diseases, screening candidate drugs, and evaluating the therapeutic effect. Here, we systematically review the general design strategies of firefly luciferin bioluminescence probes and their applications. Bioluminescence probes provide a new approach for facilitating investigation in a diverse range of fields. It inspires us to explore more robust light emission luciferin and novel design strategies to develop bioluminescent probes.

Organic & Biomolecular Chemistry published new progress about 2591-17-5. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application of C11H8N2O3S2.

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

Xiao, Qiong; Wang, Li-Ping; Jiao, Xiao-Zhen; Liu, Xiao-Yu; Wu, Qian; Xie, Ping published the artcile< Concise total synthesis of largazole>, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate, the main research area is largazole cyclic peptide enantioselective synthesis stereoselective aldol addition; thiazolidinethione chiral auxiliary stereoselective aldol addition largazole enantioselective synthesis; macrolactamization largazole cyclic peptide enantioselective synthesis.

The concise total synthesis of largazole (I) was accomplished. The key step included the use of the Nagao thiazolidinethione auxiliary for a diastereoselective acetate aldol reaction, and it acts as an acylating agent for peptide formation.

Journal of Asian Natural Products Research published new progress about Aldol addition, stereoselective. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate.

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

Luo, Jinqiu; Yang, Jinfeng; Li, Guangjie; Yang, Sheng; Zhou, Yibo; Li, Jun-Bin; Huang, Ge; Hu, Yibo; Zou, Shuangfa; Zeng, Qinghai; Yang, Ronghua published the artcile< Noncovalently Caged Firefly Luciferins Enable Amplifiable Bioluminescence Sensing of Hyaluronidase-1 Activity in Vivo>, Product Details of C11H8N2O3S2, the main research area is noncovalently caged firefly luciferins bioluminescence sensor hyaluronidase 1; bioluminescence; enzymatic assay; hyaluronidase; in vivo bioimaging; nanosensor; signal amplification.

Hyaluronidase 1 (Hyal-1) is an important enzyme involved in intracellular hyaluronic acid (HA) catabolism for performing various physiol. functions, and its aberrant level is closely associated with many malignant diseases. Bioluminescence imaging is advantageous for monitoring Hyal-1 activity in vivo, but it remains challenging to design an available probe for differentiating Hyal-1 from other isoforms by a traditional strategy that covalently masks the firefly luciferase substrate. Herein, we, for the first time, present a noncovalently caging approach to construct a Hyal-1-specific bioluminogenic nanosensor by entrapping D-luciferin (D-Luc) inside the cholesterylamine-modified HA (CHA) nanoassembly to inhibit the bioluminescence production When encountered with intracellular Hyal-1, CHA could be fully dissembled to liberate multiple copies of the loaded D-Luc, thereby emitting light by the luciferase-catalyzed bioluminescence reaction. Because of its cascade signal amplification feature, D-Luc@CHA displayed a remarkable “”turn-on”” response (248-fold) to 5μg/mL Hyal-1 with a detection limit of 0.07 ng/mL. Importantly, bioluminescence imaging results validated that D-Luc@CHA could be competent for dynamically visualizing endogenous Hyal-1 changes in living cells and animals and possessed the capability of discriminating between normal and cancer cells, thus offering a promising toolbox to evaluate Hyal-1 roles in biol. processes as well as to diagnose Hyal-1-related diseases.

ACS Sensors published new progress about Bioluminescent imaging. 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

Lopez, Vittoria; Lee, Sang-Yong; Stephan, Holger; Mueller, Christa E. published the artcile< Recombinant expression of ecto-nucleotide pyrophosphatase/phosphodiesterase 4 (NPP4) and development of a luminescence-based assay to identify inhibitors>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is human ecto nucleotide pyrophosphatase phosphodiesterase NPP4 assay inhibitor polyphosphate; Antithrombotic drug; Assay development; Ectonucleotidase; High-throughput screening; Luminescence detection; NPP4 inhibitors; Recombinant enzyme expression.

Nucleotide pyrophosphatase/phosphodiesterase 4 (NPP4) is a membrane-bound enzyme that hydrolyzes extracellular diadenosine polyphosphates such as diadenosine triphosphate (Ap3A) and diadenosine tetraphosphate (Ap4A) yielding mononucleotides. NPP4 on the surface of endothelial cells was reported to promote platelet aggregation by hydrolyzing Ap3A to ADP, which activates pro-thrombotic G protein-coupled P2Y1 and P2Y12 receptors. Thus, NPP4 inhibitors have potential as novel antithrombotic drugs. In the present study we expressed soluble human NPP4 in Sf9 insect cells and established an enzyme assay using diadenosine tetraphosphate (Ap4A) as a substrate. The reaction product ATP was quantified by luciferin-luciferase reaction in a 96-well plate format. The sensitive method displayed a limit of detection (LOD) of 14.6 nM, and a Z′-factor of 0.68 indicating its suitability for high-throughput screening. The new assay was applied for studying enzyme kinetics and led to the identification of the first NPP4 inhibitors.

Analytical Biochemistry published new progress about Antithrombotics. 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

Helmer, Rebecca A.; Martinez-Zaguilan, Raul; Kaur, Gurvinder; Smith, Lisa A.; Dufour, Jannette M.; Chilton, Beverly S. published the artcile< Helicase-like transcription factor-deletion from the tumor microenvironment in a cell line-derived xenograft model of colorectal cancer reprogrammed the human transcriptome-S-nitroso-proteome to promote inflammation and redirect metastasis>, Category: thiazole, the main research area is helicase transcription factor colorectal cancer inflammation redirect metastasis.

Methylation of the HLTF gene in colorectal cancer (CRC) cells occurs more frequently in men than women. Progressive epigenetic silencing of HLTF in tumor cells is accompanied by negligible expression in the tumor microenvironment (TME). Cell line-derived xenografts (CDX) were established in control (Hltf+/+) and Hltf-deleted male Rag2-/-IL2rg-/- mice by direct orthotopic cell microinjection (OCMI) of HLTF+/+HCT116 Red-FLuc cells into the submucosa of the cecum. Combinatorial induction of IL6 and S100A8/A9 in the Hltf-deleted TME with ICAM-1and IL8 in the primary tumor activated a pos. feedback loop. The proinflammatory niche produced a major shift in CDX metastasis to peritoneal dissemination compared to controls. Inducible nitric oxide (iNOS) gene expression and transactivation of the iNOS-S100A8/A9 signaling complex in Hltf-deleted TME reprogrammed the human S-nitroso-proteome. POTEE, TRIM52 and UN45B were S-nitrosylated on the conserved I/L-X-C-X2-D/E motif indicative of iNOS-S100A8/A9-mediated S-nitrosylation. 2D-DIGE and protein identification by MALDI-TOF/TOF mass spectrometry authenticated S-nitrosylation of 53 individual cysteines in half-site motifs (I/L-X-C or C-X-X-D/E) in CDX tumors. POTEE in CDX tumors is both a general S-nitrosylation target and an iNOS-S100A8/A9 site-specific (Cys638) target in the Hltf-deleted TME. REL is an example of convergence of transcriptomic-S-nitroso-proteomic signaling. The gene is transcriptionally activated in CDX tumors with an Hltf-deleted TME, and REL-SNO (Cys143) was found in primary CDX tumors and all metastatic sites. Primary CDX tumors from Hltf-deleted TME shared 60% of their S-nitroso-proteome with all metastatic sites. Forty percent of SNO-proteins from primary CDX tumors were variably expressed at metastatic sites. Global S-nitrosylation of proteins in pathways related to cytoskeleton and motility was strongly implicated in the metastatic dissemination of CDX tumors. Hltf-deletion from the TME played a major role in the pathogenesis of inflammation and linked protein S-nitrosylation in primary CDX tumors with spatiotemporal continuity in metastatic progression when the tumor cells expressed HLTF.

PLoS One published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (POTEE). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Category: thiazole.

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

Saputra, Elizabeth P.; Trzeciakowski, Jerome P.; Hyde, Jenny A. published the artcile< Borrelia burgdorferi spatiotemporal regulation of transcriptional regulator bosR and decorin binding protein during murine infection>, Related Products of 2591-17-5, the main research area is Borrelia burgdorferi bosR decorin binding protein murine infection.

Lyme disease, caused by Borrelia burgdorferi, is an inflammatory multistage infection, consisting of localized, disseminated, and persistent disease stages, impacting several organ systems through poorly defined gene regulation mechanisms. The purpose of this study is to further characterize the spatiotemporal transcriptional regulation of B. burgdorferi during mammalian infection of borrelial oxidative stress regulator (bosR) and decorin binding protein (dbpBA) by utilizing bioluminescent B. burgdorferi reporter strains and in vivo imaging. Fluctuating borrelial load was also monitored and used for normalization to evaluate expression levels. BosR transcription is driven by two promoters, Pbb0648 and PbosR, and we focused on the native promoter. BosR expression is low relative to the robustly expressed dbpBA throughout infection. In distal tissues, bosR was the highest in the heart during in the first week whereas dbpBA was readily detectable at all time points with each tissue displaying a distinct expression pattern. This data suggests bosR may have a role in heart colonization and the induction of dbpBA indicates a RpoS independent transcriptional regulation occurring in the mammalian cycle of pathogenesis. These finding demonstrate that B. burgdorferi engages unknown genetic mechanisms to uniquely respond to mammalian tissue environments and/or changing host response over time.

Scientific Reports published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Related Products of 2591-17-5.

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

Calabretta, Maria Maddalena; Alvarez-Diduk, Ruslan; Michelini, Elisa; Roda, Aldo; Merkoci, Arben published the artcile< Nano-lantern on paper for smartphone-based ATP detection>, Quality Control of 2591-17-5, the main research area is adenosine triphosphate biosensor smartphone paper urinary tract infection; ATP biosensor; Bioluminescence; Luciferase; Paper-based biosensor; Smartphone.

ATP-driven bioluminescence relying on the D-luciferin-luciferase reaction is widely employed for several biosensing applications where bacterial ATP detection allows to verify microbial contamination for hygiene monitoring in hospitals, food processing and in general for cell viability studies. Several ATP kit assays are already com. available but an user-friendly ATP biosensor characterized by low-cost, portability, and adequate sensitivity would be highly valuable for rapid and facile on site screening. Thanks to an innovative freeze-drying procedure, we developed a user-friendly, ready-to-use and stable ATP sensing paper biosensor that can be combined with smartphone detection. The ATP sensing paper includes a lyophilized “”nano-lantern”” with reaction components being rapidly reconstituted by 10μL sample addition, enabling detection of 10-14 mol of ATP within 10 min. We analyzed urinary microbial ATP as a biomarker of urinary tract infection (UTI), confirming the capability of the ATP sensing paper to detect the threshold for positivity corresponding to 105 colony-forming units of bacteria per mL of urine.

Biosensors & Bioelectronics published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Quality Control of 2591-17-5.

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

Liu, Jingjing; Tian, Zhenwei; Liu, Tianzhou; Wen, Dacheng; Ma, Zhiming; Liu, Yuanda; Zhu, Jiaming published the artcile< CHSY1 is upregulated and acts as tumor promotor in gastric cancer through regulating cell proliferation, apoptosis, and migration>, Quality Control of 2591-17-5, the main research area is prognosis CHSY1 XIAP cell proliferation migration metastatic gastric cancer; CHSY1; Gastric cancer; cell apoptosis; cell migration; cell proliferation.

Gastric cancer is one of the most frequently diagnosed malignant tumors, with rapid progression and poor prognosis. The role of chondroitin sulfate synthase 1 (CHSY1) in the development and progression of gastric cancer was explored and clarified in this study. The immunohistochem. anal. of clin. tissue samples as well as data mining of public database showed that CHSY1 was significantly upregulated in gastric cancer and associated with more advanced tumor stage and poorer prognosis. In vitro loss-of-function experiments demonstrated the inhibited cell proliferation, colony formation, cell migration, as well as the promoted cell apoptosis by CHSY1 knockdown. Moreover, recovery of CHSY1 expression could attenuate the regulatory effects induced by CHSY1 knockdown. Correspondingly, gastric cancer cells with CHSY1 knockdown showed reduced tumorigenicity and slower tumor growth in vivo. In conclusion, this study identified CHSY1 as a tumor promotor in gastric cancer, which may be utilized as a novel indicator of patients′ prognosis and therapeutic target for developing more effective drug for GC treatment.

Cell Cycle published new progress about Apoptosis. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Quality Control of 2591-17-5.

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

Hansen, Ida K. O.; Loevdahl, Tomas; Simonovic, Danijela; Hansen, Kine O.; Andersen, Aaron J. C.; Devold, Hege; Richard, C. Eline S. M.; Andersen, Jeanette H.; Strom, Morten B.; Haug, Tor published the artcile< Antimicrobial activity of small synthetic peptides based on the marine peptide turgencin a: prediction of antimicrobial peptide sequences in a natural peptide and strategy for optimization of potency>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is turgencin antimicrobial peptide Escherichia Staphylococcus; Arctic; Synoicum turgens; antimicrobial; ascidian; peptide; synthetic.

Turgencin A, a potent antimicrobial peptide isolated from the Arctic sea squirt Synoicum turgens, consists of 36 amino acid residues and three disulfide bridges, making it challenging to synthesize. The aim of the present study was to develop a truncated peptide with an antimicrobial drug lead potential based on turgencin A. The experiments consisted of: (1) sequence anal. and prediction of antimicrobial potential of truncated 10-mer sequences; (2) synthesis and antimicrobial screening of a lead peptide devoid of the cysteine residues; (3) optimization of in vitro antimicrobial activity of the lead peptide using an amino acid replacement strategy; and (4) screening the synthesized peptides for cytotoxic activities. In silico anal. of turgencin A using various prediction software indicated an internal, cationic 10-mer sequence to be putatively antimicrobial. The synthesized truncated lead peptide displayed weak antimicrobial activity. However, by following a systematic amino acid replacement strategy, a modified peptide was developed that retained the potency of the original peptide. The optimized peptide StAMP-9 displayed bactericidal activity, with minimal inhibitory concentrations of 7.8 μg/mL against Staphylococcus aureus and 3.9 μg/mL against Escherichia coli, and no cytotoxic effects against mammalian cells. Preliminary experiments indicate the bacterial membranes as immediate and primary targets.

International Journal of Molecular Sciences published new progress about Anti-inflammatory agents. 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

Liu, Tracy W.; Gammon, Seth T.; Fuentes, David; Piwnica-Worms, David published the artcile< Multi-modal multi-spectral intravital macroscopic imaging of signaling dynamics in real time during tumor-immune interactions>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is bioluminescence; imaging reporters; immune cell imaging; intravital imaging; molecular imaging; tumor signaling; tumor–immune interactions.

A major obstacle in studying the interplay between cancer cells and the immune system has been the examination of proposed biol. pathways and cell interactions in a dynamic, physiol. relevant system in vivo. Intravital imaging strategies are one of the few mol. imaging techniques that can follow biol. processes at cellular resolution over long periods of time in the same individual. Bioluminescence imaging has become a standard preclin. in vivo optical imaging technique with ever-expanding versatility as a result of the development of new emission bioluminescent reporters, advances in genomic techniques, and tech. improvements in bioluminescence imaging and processing methods. Herein, we describe an advance of technol. with a mol. imaging window chamber platform that combines bioluminescent and fluorescent reporters with intravital macro-imaging techniques and bioluminescence spectral unmixing in real time applied to heterogeneous living systems in vivo for evaluating tumor signaling dynamics and immune cell enzyme activities concurrently.

Cells published new progress about 2591-17-5. 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