Category: 2591-17-5

Zhao, Pei; Wu, Xiaokang; Li, Jie; Dong, Gaopan; Sun, Yingai; Ma, Zhao; Li, Minyong; Du, Lupei published the artcile< Discovery of alkene-conjugated luciferins for redshifted and improved bioluminescence imaging in vitro and in vivo>, Formula: C11H8N2O3S2, the main research area is .

The firefly luciferase system is the most extensively utilized bioluminescence system in the field of life science at the moment. In this work, we designed and synthesized a series of alkene-conjugated luciferins to develop new firefly bioluminescence substrates, and further evaluated their activities in vitro and in vivo. It is worth noting that the maximum biol. emission wavelength of novel luciferin analog AL3 ((S,E)-2-(6-hydroxy-5-(3-methoxy-3-oxoprop-1-en-1-yl)benzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid) is 100 nm red-shifted compared with D-luciferin, while that of analog AL4 ((S,E)-2-(5-(2-cyanovinyl)-6-hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid) is 75 nm red-shifted. The new substrate AL2 ((S,E)-2-(6-hydroxy-7-(3-methoxy-3-oxoprop-1-en-1-yl)benzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid) showed better bioluminescence performance in vivo.

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

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

Inouye, Satoshi; Nakamura, Mitsuhiro; Taguchi, Jumpei; Hosoya, Takamitsu published the artcile< Identification of a novel oxidation product from yellow fluorophore in the complex of apoPholasin and dehydrocoelenterazine>, Application of C11H8N2O3S2, the main research area is oxidation yellow fluorophore complex apoPholasin dehydrocoelenterazine; Coelenteramide; Coelenteramine; Coelenterazine; Photoproteins; Reactive oxygen.

The complex of the recombinant fusion protein of apoPholasin and glutathione S-transferase (GST-apoPholasin) with non-fluorescent dehydrocoelenterazine (dCTZ) (GST-apoPholasin/dCTZ complex) shows yellow fluorescence at 539 nm by excitation at 430 nm. The GST-apoPholasin/dCTZ complex with a fluorophore (dCTZ*) has considerably weak luminescence activity, converting slowly to a blue fluorescence protein with the emission peak at 430 nm. The main oxidation products from dCTZ* for blue fluorescence were identified as coelenteramine (CTM) and an unreported pyrazine derivative, 3-benzyl-5-(4-hydroxyphenyl)pyrazin-2(1H)-one (CTO) that was confirmed by chem. synthesis.

Bioorganic & Medicinal Chemistry Letters published new progress about Chimeric fusion proteins Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (GST-apoPholasin). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application of C11H8N2O3S2.

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

Ji, Xincai; Adams, Spencer T. Jr.; Miller, Stephen C. published the artcile< Bioluminescence imaging in mice with synthetic luciferin analogues>, Computed Properties of 2591-17-5, the main research area is review bioluminescence imaging synthetic luciferin analog transgenic mice; AAV; Coelenterazine; CycLuc1; FAAH; Firefly; GFAP; Luciferase; NanoLuc; PHP.eB; Transgenic.

A review. Luciferase enzymes from bioluminescent organisms can be expressed in mice, enabling these rodents to glow when treated with a corresponding luciferin substrate. Light emission occurs where the expression of the genetically-encoded luciferase overlaps with the biodistribution of the administered small mol. luciferin. Here we discuss differences between firefly luciferin analogs for bioluminescence imaging, focusing on transgenic and adeno-associated virus (AAV)-transduced mice.

Methods in Enzymology published new progress about Adeno-associated virus. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Computed Properties of 2591-17-5.

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

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

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

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

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

Moriguchi, Maiko; Takahashi, Ryo; Kang, Bubwoong; Kuse, Masaki published the artcile< Expression of recombinant apopholasin using a baculovirus-silkworm multigene expression system and activation via dehydrocoelenterazine>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is expression recombinant apopholasin baculovirus silkworm multigene system activation dehydrocoelenterazine; Apopholasin; Baculovirus–silkworm multigene expression system; Chromophore; Dehydrocoelenterazine; Pholasin.

Pholasin is a photoprotein derived from the glowing bivalve mollusk, Pholas dactylus. Even though the chem. structure of the prosthetic group (chromophore) responsible for the light emission character of the mollusk remains unknown, research showed that the presence of dehydrocoelenterazine (DCL) increased light emission and that the dithiothreitol adduct of DCL was isolated from Pholasin. To date, the authors’ research has been focused on activating apopholasin, the naturally occurring apoprotein of Pholasin, using DCL. In the current study, the expression of recombinant apopholasin via a baculovirus-silkworm multigene expression system is reported. Addnl., the purification of apopholasin using a Flag-affinity column, the activation of apopholasin using DCL, and the initiation of its luminescent character through the addition of a peroxidase-hydrogen peroxide mixture are reported. The peroxidase-H2O2-dependent luminescence was observed from the recombinant apopholasin activated with DCL.

Bioorganic & Medicinal Chemistry Letters 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

Tan, Richard P.; Hallahan, Nicole; Kosobrodova, Elena; Michael, Praveesuda L.; Wei, Fei; Santos, Miguel; Lam, Yuen Ting; Chan, Alex H. P.; Xiao, Yin; Bilek, Marcela M. M.; Thorn, Peter; Wise, Steven G. published the artcile< Bioactivation of Encapsulation Membranes Reduces Fibrosis and Enhances Cell Survival>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is islet encapsulation device immunomodulatory surface coating macrophage polarization; encapsulation devices; immunomodulatory surface coatings; islet cells; macrophage polarization; type I diabetes.

Encapsulation devices are an emerging barrier technol. designed to prevent the immunorejection of replacement cells in regenerative therapies for intractable diseases. However, traditional polymers used in current devices are poor substrates for cell attachment and induce fibrosis upon implantation, impacting long-term therapeutic cell viability. Bioactivation of polymer surfaces improves local host responses to materials, and here we make the first step toward demonstrating the utility of this approach to improve cell survival within encapsulation implants. Using therapeutic islet cells as an exemplar cell therapy, we show that internal surface coatings improve islet cell attachment and viability, while distinct external coatings modulate local foreign body responses. Using plasma surface functionalization (plasma immersion ion implantation (PIII)), we employ hollow fiber semiporous poly(ether sulfone) (PES) encapsulation membranes and coat the internal surfaces with the extracellular matrix protein fibronectin (FN) to enhance islet cell attachment. Sep., the external fiber surface is coated with the anti-inflammatory cytokine interleukin-4 (IL-4) to polarize local macrophages to an M2 (anti-inflammatory) phenotype, muting the fibrotic response. To demonstrate the power of our approach, bioluminescent murine islet cells were loaded into dual FN/IL-4-coated fibers and evaluated in a mouse back model for 14 days. Dual FN/IL-4 fibers showed striking reductions in immune cell accumulation and elevated levels of the M2 macrophage phenotype, consistent with the suppression of fibrotic encapsulation and enhanced angiogenesis. These changes led to markedly enhanced islet cell survival and importantly to functional integration of the implant with the host vasculature. Dual FN/IL-4 surface coatings drive multifaceted improvements in islet cell survival and function, with significant implications for improving clin. translation of therapeutic cell-containing macroencapsulation implants.

ACS Applied Materials & Interfaces published new progress about Angiogenesis. 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