Tag: M.W=250-300

Ye, Sen; Hananya, Nir; Green, Ori; Chen, Hansen; Zhao, Angela Qian; Shen, Jiangang; Shabat, Doron; Yang, Dan published the artcile< A Highly Selective and Sensitive Chemiluminescent Probe for Real-Time Monitoring of Hydrogen Peroxide in Cells and Animals>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is Chemiluminescent probe hydrogen peroxide bioimaging imaging agent; bioimaging; chemiluminescence; fluorescent probes; hydrogen peroxide; imaging agents.

Selective and sensitive mol. probes for hydrogen peroxide (H2O2), which plays diverse roles in oxidative stress and redox signaling, are urgently needed to investigate the physiol. and pathol. effects of H2O2. A lack of reliable tools for in vivo imaging has hampered the development of H2O2 mediated therapeutics. By combining a specific tandem Payne/Dakin reaction with a chemiluminescent scaffold, H2O2-CL-510 was developed as a highly selective and sensitive probe for detection of H2O2 both in vitro and in vivo. A rapid 430-fold enhancement of chemiluminescence was triggered directly by H2O2 without any laser excitation. Arsenic trioxide induced oxidative damage in leukemia was successfully detected. In particular, cerebral ischemia-reperfusion injury-induced H2O2 fluxes were visualized in rat brains using H2O2-CL-510, providing a new chem. tool for real-time monitoring of H2O2 dynamics in living animals.

Angewandte Chemie, International Edition published new progress about Biological imaging. 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

Bernier, Jean Luc; Houssin, Raymond; Henichart, Jean Pierre published the artcile< Analog of dolastatin 3. Synthesis, proton NMR studies, and spatial conformation>, COA of Formula: C12H18N2O4S, the main research area is dolastatin 3 analog preparation conformation.

Dolastatin 3 analog I was prepared by deblocking Boc-Pro-Leu-Val-(gly)Thz-(gly)Thz-ONSu (II; Boc = Me3CO2C, NSu = succinimido) by HBr/HOAc and cyclizing the resulting H-Pro-Leu-Val-(gly)Thz-(gly)Thz-ONSu.HBr in pyridine. Boc-Gly-NH2 underwent thionation via the Lawesson procedure to give Boc-Gly(S)-NH2, which was cyclized with CH3COCO2Et to give Boc-(gly)Thz-OEt (III). III was Boc-deblocked by HBr/HOAc to give H-(gly)Thz-OEt.HBr (IV), whereas III was saponified to give Boc-(gly)Thz-OH (V). V was coupled with IV by DCC/HOBt to give Boc-(gly)Thz-(gly)Thz-OEt, which was Boc-deblocked and then coupled with Boc-Pro-Leu-Val-OH by DCC/HOBt to give Boc-Pro-Leu-Val-(gly)Thz-(gly)Thz-OEt, which was converted into II. A spatial mol. conformation of I was proposed based on 1H NMR spectroscopy.

Tetrahedron published new progress about Cyclic peptides Role: SPN (Synthetic Preparation), PREP (Preparation). 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, COA of Formula: C12H18N2O4S.

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

Chen, Liying; Chen, Zhi; Zheng, Shuang; Fan, Luhui; Zhu, Lixin; Yu, Jiandong; Tang, Chaoyuan; Liu, Qi; Xiong, Yang published the artcile< Study on mechanism of elemene reversing tumor multidrug resistance based on luminescence pharmacokinetics in tumor cells in vitro and in vivo>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is elemene reversing tumor multidrug resistance luminescence pharmacokinetics.

While elemene (ELE) can reverse tumor multidrug resistance (MDR), the mechanisms for ELE reversing MDR remain unclear. Numerous studies have suggested that the efflux functionality of ATP-binding cassette (ABC) transporters, not their quantity, is more relevant to tumor MDR. However, no appropriate methods exist for real-time detection of the intracellular drug efflux caused by ABC transporters in vitro, especially in vivo, which hinders the examination of MDR reversal mechanisms. This study directly investigates the correlation between efflux functionality of ABC transporters and MDR reversal via ELE, using D-luciferin potassium salt (D-luc) as the chemotherapeutic substitute to study the intracellular drug efflux. Here, a luciferase reporter assay system combined with bioluminescence imaging confirmed that the efflux of D-luc from MCF-7/DOXFluc cells in vitro and in vivo was significantly reduced by ELE and when combined with Doxorubicin (DOX), ELE showed a synergistically anti-tumor effect in vitro and in vivo. Addnl., the luminescence pharmacokinetics of D-luc in MCF-7/DOXFluc cells and pharmacodynamics of the combined ELE and DOX in vivo showed a great correlation, implying that D-luc might be used as a probe to study ABC transporters-mediated efflux in order to explore mechanisms of traditional Chinese medicines reversing MDR.

RSC Advances 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

Nakayama, Jun; Saito, Ryohei; Hayashi, Yusuke; Kitada, Nobuo; Tamaki, Shota; Han, Yuxuan; Semba, Kentaro; Maki, Shojiro A. published the artcile< High sensitivity in vivo imaging of cancer metastasis using a near-infrared luciferin analogue seMpai>, Application In Synthesis of 2591-17-5, the main research area is cancer metastasis IR luciferin analog sempai; in vivo imaging; luciferin analogue; metastasis; near-infrared bioluminescence.

Bioluminescence imaging (BLI) is useful to monitor cell movement and gene expression in live animals. However, D-luciferin has a short wavelength (560 nm) which is absorbed by tissues and the use of near-IR (NIR) luciferin analogs enable high sensitivity in vivo BLI. The AkaLumine-AkaLuc BLI system (Aka-BLI) can detect resolution at the single-cell level; however, it has a clear hepatic background signal. Here, to enable the highly sensitive detection of bioluminescence from the surrounding liver tissues, we focused on seMpai (C15H16N3O2S) which has been synthesized as a luciferin analog and has high luminescent abilities as same as AkaLumine. We demonstrated that seMpai BLI could detect micro-signals near the liver without any background signal. The solution of seMpai was neutral; therefore, seMpai imaging did not cause any adverse effect in mice. seMpai enabled a highly sensitive in vivo BLI as compared to previous techniques. Our findings suggest that the development of a novel mutated luciferase against seMpai may enable a highly sensitive BLI at the single-cell level without any background signal. Novel seMpai BLI system can be used for in vivo imaging in the fields of life sciences and medicine.

International Journal of Molecular Sciences published new progress about Bioluminescent imaging. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application In Synthesis of 2591-17-5.

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

Murty, Surya; Haile, Samuel T.; Beinat, Corinne; Aalipour, Amin; Alam, Israt S.; Murty, Tara; Shaffer, Travis M.; Patel, Chirag B.; Graves, Edward E.; Mackall, Crystal L.; Gambhir, Sanjiv S. published the artcile< Intravital imaging reveals synergistic effect of CAR T-cells and radiation therapy in a preclinical immunocompetent glioblastoma model>, HPLC of Formula: 2591-17-5, the main research area is disialoganglioside GD2 CAR T cell apoptosis glioblastoma; Chimeric antigen receptor (CAR); glioblastoma; imaging; immunotherapy; intravital microscopy.

Recent advances in novel immune strategies, particularly chimeric antigen receptor (CAR)-bearing T-cells, have shown limited efficacy against glioblastoma (GBM) in clin. trials. We currently have an incomplete understanding of how these emerging therapies integrate with the current standard of care, specifically radiation therapy (RT). Addnitionally, there is an insufficient number of preclin. studies monitoring these therapies with high spatiotemporal resolution To address these limitations, we report the first longitudinal fluorescence-based intravital microscopy imaging of CAR T-cells within an orthotopic GBM preclin. model to illustrate the necessity of RT for complete therapeutic response. Complete antitumor response in advanced syngeneic orthotopic models of GBM was achieved only when a single i.v. dose of GD2 CAR T-cells was following either sub-lethal whole-body irradiation or focal RT. Intravital microscopy imaging successfully visualized CAR T-cell homing and T-cell mediated apoptosis of tumor cells in real-time within the tumor stroma. Findings indicate that RT allows for rapid CAR T-cell extravasation from the vasculature and expansion within the tumor microenvironment. These exciting results highlight potential opportunities to improve IV adoptive T-cell administration in the treatment of GBM through concurrent RT. Addnl., they emphasize the need for advancements in immunotherapeutic homing to and extravasation through the tumor microenvironment.

OncoImmunology published new progress about Apoptosis. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, HPLC of Formula: 2591-17-5.

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

Patel, Bhargav A.; Abel, Biebele; Barbuti, Anna Maria; Velagapudi, Uday Kiran; Chen, Zhe-Sheng; Ambudkar, Suresh V.; Talele, Tanaji T. published the artcile< Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein>, Safety of Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate, the main research area is thiazole peptidomimetic synthesis ATPase stimulator inhibitor structure activity; drug substrate binding P glycoprotein antitumor agent mol docking; peptide coupling Boc protection.

A novel set of 64 analogs based on our lead compound (I) was designed and synthesized with an initial objective of understanding the structural requirements of ligands binding to a highly perplexing substrate-binding site of P-gp and their effect on modulating the ATPase function of the efflux pump. Compound I, a stimulator of P-gp ATPase activity, was transformed to ATPase inhibitory compounds (II), (III) and (IV). The ATPase inhibition by these compounds was predominantly contributed by the presence of a cyclohexyl group in lieu of the 2-aminobenzophenone moiety of I. The 4,4-difluorocyclohexyl analogs III and IV inhibited the photolabeling by [125I]-IAAP, with IC50 values of 0.1 and 0.76 M, resp. Selected compounds were shown to reverse paclitaxel resistance in HEK293 cells overexpressing P-gp and were selective toward P-gp over CYP3A4. Induced-fit docking highlighted a plausible binding pattern of inhibitory compounds in the putative-binding pocket of P-gp. The current study underscores the stringent requirement by P-gp to bind to chem. similar mols.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Safety of Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate.

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

Nakajima, Kanako; Hamada, Kazuko; Ito, Ryoga; Yoshida, Yukina; Sutherland, Kenneth; Ishikawa, Masayori; Ozaki, Michitaka; Shirato, Hiroki; Hamada, Toshiyuki published the artcile< Stability of -luciferin for bioluminescence to detect gene expression in freely moving mice for long durations>, Product Details of C11H8N2O3S2, the main research area is Dluciferin L luciferin antiobesity agent obesity cancer; Period1; circadian rhythm; in vivo imaging; luciferin.

Circadian disturbance of clock gene expression is a risk factor for diseases such as obesity, cancer, and sleep disorders. To study these diseases, it is necessary to monitor and analyze the expression rhythm of clock genes in the whole body for a long duration. The bioluminescent reporter enzyme firefly luciferase and its substrate -luciferin have been used to generate optical signals from tissues in vivo with high sensitivity. However, little information is known about the stability of -luciferin to detect gene expression in living animals for a long duration. In the present study, we examined the stability of a luciferin solution over 21 days. -Luciferin, which is synthesized using racemization of -luciferin, was at high concentrations after 21 days. In addition, we showed that bioluminescence of Period1 (Per1) expression in the liver was significantly decreased compared with the day 1 solution, although locomotor activity rhythm was not affected. These results showed that -luciferin should be applied to the mouse within, at most, 7 days to detect bioluminescence of Per1 gene expression rhythm in vivo.

Luminescence published new progress about Acyl-CoA-binding 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

Shrestha, Tej B.; Basel, Matthew T. published the artcile< Using Naturally Occurring Bioluminescent Enzymes to Track Specific Cell Populations>, SDS of cas: 2591-17-5, the main research area is review natural bioluminescent enzyme cell population tracking; Bioluminescence; Luminol; Myeloperoxidase; NADPH oxidase; Neutrophil.

A review. Luminol-based bioluminescence imaging allows noninvasive tracking of oxidatively active cells such as neutrophils. Luminol is given i.v. or i.p., followed by bioluminescence imaging at 425 nm. Here we describe a method for tracking neutrophil extravasation into an inflammatory site, especially focusing on mammary carcinoma.

Methods in Molecular Biology (New York, NY, United States) published new progress about Bioluminescent imaging. 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

Chen, Tzu-Yin; Chen, Mei-Ru; Liu, Shan-Wen; Lin, Jin-Yan; Yang, Ya-Ting; Huang, Hsin-Ying; Chen, Jen-Kun; Yang, Chung-Shi; Lin, Kurt Ming-Chao published the artcile< Assessment of polyethylene glycol-coated gold nanoparticle toxicity and inflammation in vivo using NF-κB reporter mice>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is polyethylene glycol coated gold nanoparticle toxicity inflammation reporter mice; NF-κB; PEG surface modification; gold nanoparticle; liver inflammation; reporter imaging; steatosis.

Polyethylene glycol (PEG) coating of gold nanoparticles (AuNPs) improves AuNP distribution via blood circulation. The use of PEG-coated AuNPs was shown to result in acute injuries to the liver, kidney, and spleen, but long-term toxicity has not been well studied. In this study, we investigated reporter induction for up to 90 days in NF-κB transgenic reporter mice following i.v. injection of PEG-coated AuNPs. The results of different doses (1 and 4μg AuNPs per g of body weight), particle sizes (13 nm and 30 nm), and PEG surfaces (methoxyl- or carboxymethyl-PEG 5 kDa) were compared. The data showed up to 7-fold NF-κB reporter induction in mouse liver from 3 h to 7 d post PEG-AuNP injection compared to saline-injected control mice, and gradual reduction to a level similar to control by 90 days. Agglomerates of PEG-AuNPs were detected in liver Kupffer cells, but neither gross pathol. abnormality in liver sections nor increased activity of liver enzymes were found at 90 days. Injection of PEG-AuNPs led to an increase in collagen in liver sections and elevated total serum cholesterol, although still within the normal range, suggesting that inflammation resulted in mild fibrosis and affected hepatic function. Administrating PEG-AuNPs inevitably results in nanoparticles entrapped in the liver; thus, further investigation is required to fully assess the long-term impacts by PEG-AuNPs on liver health.

International Journal of Molecular Sciences published new progress about Hepatotoxicity. 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

Schneider, Tanya L.; Walsh, Christopher T.; O’Connor, Sarah E. published the artcile< Utilization of Alternate Substrates by the First Three Modules of the Epothilone Synthetase Assembly Line>, Product Details of C12H18N2O4S, the main research area is substrate specificity epothilone synthetase Sorangium serine polyketide oxazole analog.

The epothilones, a family of macrolactone natural products produced by the myxobacterial species Sorangium cellulosum, are of current clin. interest as antitumor agents. Inspection of the structure of the epothilones suggests a hybrid polyketide/nonribosomal peptide biosynthetic origin, and the recent sequencing of the epothilone biosynthetic gene cluster has validated this proposal. Here we have examined unnatural substrates with the first two enzymes of the biosynthetic pathway, EpoA and EpoB, to investigate the enzymic construction of alternate heterocyclic structures and the subsequent elongation of these products by the third enzyme of the pathway, EpoC. The epothilone biosynthetic machinery can utilize serine to install an oxazole in place of a thiazole in the epothilone structure and will tolerate functionalized donor groups from the EpoA-ACP domain to produce epothilone fragments modified at the C21 position. These studies with the early enzymes of the epothilone biosynthesis cluster suggest that combinatorial biosynthesis may be a viable means for producing a variety of epothilone analogs that incorporate diversity into the heterocycle starter unit.

Journal of the American Chemical Society published new progress about Sorangium cellulosum. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Product Details of C12H18N2O4S.

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