Search results for: CF350 maleimide
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Alterations in conformational state of albumin in plasma in chronic hemodialyzed patients.In chronic hemodialyzed (CH) patients the balance between production of reactive oxygen species and antioxidant defense system is disturbed and shifted towards oxidative conditions. The properties of albumin in CH patients were studied before hemodialysis (HD) and post-HD.
2405 related Products with: Alterations in conformational state of albumin in plasma in chronic hemodialyzed patients.Anti 3 DG imidazolone Mon Lipoproteins, Human Plasm Human interleukin 2(IL-2) Bovine prolactin-induced Plasma Proteins: Corn Try Rabbit Plasma US Origin I Rabbit Plasma US Origin I Rabbit Plasma US Origin I Rabbit Plasma US Origin I Rabbit Plasma US Origin I Rabbit Plasma US Origin I Rabbit Plasma US Origin I
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Bioresponsive albumin-conjugated paclitaxel prodrugs for cancer therapy.The efficacy of traditional chemotherapy often suffers from rapid clearance and off-target toxicity. Drug delivery systems and controlled release are applied to improve the therapeutic efficiencies of small-molecule drugs. In this work, two novel oxidative/reductive (Ox/Re) -sensitive and one non-sensitive Paclitaxel (PTX) prodrugs were synthesized with a maleimide group, which rapidly conjugates with albumin in vivo. Albumin serves as a good vehicle to deliver more prodrug to tumors due to the enhanced permeation and retention (EPR) effect. PTX was then released from the prodrugs in glutathione(GSH)/ reactive oxygen species(ROS)-rich tumor microenvironments. This bioresponsive prodrug strategy demonstrates potent chemotherapeutic efficiency in vivo and may be utilized in clinical cancer therapy.
1365 related Products with: Bioresponsive albumin-conjugated paclitaxel prodrugs for cancer therapy.Anti-BOVINE ALBUMIN Bioti Anti BOVINE ALBUMIN Bioti Anti-BOVINE ALBUMIN Fluor Anti BOVINE ALBUMIN Fluor Anti-BOVINE ALBUMIN Perox Anti BOVINE ALBUMIN Perox Cellufine Formyl , 50 ml Cellufine Formyl Media Cellufine Formyl , 500 ml Cellufine Formyl Media Cellufine Formyl Media CA125, Ovarian Cancer An
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Impact of site-specific conjugation of scFv to multifunctional nanomedicines using second generation maleimide.Biocompatible multifunctional nanomedicines (NMs) are known to be an attractive platform for targeted anticancer theranosis. However, these nanomedicines have an interest only if they efficiently target diseased cells and accumulate in tumors. Here we report the synthesis of a new generation of immunotargeted nanomedicines composed of a superparamagnetic iron oxide nanoparticle (SPION) core, polyethylene glycol coating and the anti-HER2 single chain fragment variable (scFv) of Trastuzumab antibody. We developed two novel bioengineered scFv carrying two cysteines located (i) at the end (4D5.1-cys2) or (ii) at the beginning (4D5.2-cys2) of its hexahistidine tag. The scFv bioconjugation was controlled via hetero-bifunctional linkers including a second generation maleimide (SGM). Our data indicated that the insertion of cysteines at the beginning of the hexahistidine tag was allowed to obtain nearly two-fold conjugation efficiency (13 scFv/NP) compared to NMs using classical maleimide. As a result, the NMs-4D5.2 built using the optimal 4D5-cys2 and linkers equipped with SGM showed the enhanced recognition of HER2 in an ELISA format and on the surface of SK-BR-3 breast cancer cells in vitro. Their stability in serum was also significantly improved compared to the NMs-4D5. Our results showed the fundamental importance of the controlled ligands conjugation in a perspective of rational design of NMs with tailored physico-chemical and biological properties.
2479 related Products with: Impact of site-specific conjugation of scFv to multifunctional nanomedicines using second generation maleimide.Ofloxacin CAS Number [824 Actin, Muscle Specific; Actin, Muscle Specific; PSA (Prostate Specific A PSA (Prostate Specific A PSAP (Prostate Specific PSAP (Prostate Specific PSA (Prostate Specific A PSA (Prostate Specific A Topoisomerase II; Clone Topoisomerase II; Clone Actin, Muscle Specific;
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Dual Maleimides Tagging for Relative and Absolute Quantitation of Cysteine-Containing Peptides by MALDI-TOF MS.A dual maleimides (DuMal) tagging method has been developed for both relative and absolute quantitation of cysteine-containing peptides (CCPs) in combination with MALDI-TOF mass spectrometry. We choose a pair of maleimides with the minimal difference in their chemical structures, including N-Methylmaleimide (NMM) and N-Ethylmaleimide (NEM), which allow for tagging CCPs in the Michael Addition reaction with a high efficiency rapidly (~minutes). We have validated that the DuMal Tagging technique is sensitive and reliable in quantitative analysis of CCPs. Absolute quantitation of CCPs can be achieved with the detection limit as low as 7.3 nM. Relative quantitation of CCPs can be performed in various sample mixtures with consistent results of the ratio (CV < 5%). The DuMal Tagging technique provides a sensitive and accurate approach for the quantitation of biomolecules containing thiol reactive sites, thus promising protein detection, disease diagnosis, and biomarker discovery associated with post-translational modifications of cysteines.
2803 related Products with: Dual Maleimides Tagging for Relative and Absolute Quantitation of Cysteine-Containing Peptides by MALDI-TOF MS.Amplite™ Fluorimetric F Cellufine Formyl , 50 ml Cellufine Formyl Media Cellufine Formyl , 500 ml Cellufine Formyl Media Cellufine Formyl Media Formalin Solution (20%) Formalin Solution (20%) Formalin Solution (20%) Formalin (10% Neutral Bu Formalin (10% Neutral Bu Zinc Formalin Solution
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Rational design of substituted maleimide dyes with tunable fluorescence and solvafluorochromism.A series of maleimide derivatives were systematically designed and synthesized with tunable fluorescent properties. The facile modifications herein provide a simple methodology to expand the scope of maleimide-based dyes and also provide insight into the relationship between substitution pattern and optical properties.
2300 related Products with: Rational design of substituted maleimide dyes with tunable fluorescence and solvafluorochromism.Amplite™ Fluorimetric M Fluorescein *Fluorescence Amplite™ Fluorimetric G Amplite™ Fluorimetric G Amplite™ Fluorimetric G Amplite™ Fluorimetric G Amplite™ Fluorimetric F iFluor™ 350 maleimide iFluor™ 488 maleimide iFluor™ 555 maleimide iFluor™ 647 maleimide iFluor™ 680 maleimide
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Orthogonally Protected Diaminoterephthalate Scaffolds: Installation of Two Functional Units at the Chromophore.The 2,5-diaminoterephthalate structural motif is a powerful chromophore with remarkable fluorescence properties. Containing two carboxylate and two amino functions, it defines a colored molecular scaffold which allows for orthogonal functionalization with different functional units. Therefore, different applications in life sciences and materials science could be addressed. In this study, the two amino functions were alkylated by reductive amination with side chains carrying amino (orthogonally protected as Boc or Alloc) and carboxylate functions (orthogonally protected as tBu or allyl ester). After sequential deprotections, functional units were introduced by amidation reactions. As three examples, the chromophore was coupled with retinoic acid and fullerene Cin order to obtain a triad for studying photoinduced electron transfer processes. Furthermore, cyclooctyne and azide moieties were introduced as functional units, allowing for ligation by click reactions. These two clickable groups were applied in combination with maleimide units which are reactive toward thiol residues. The latter dyes define so-called "turn on" probes, since the fluorescence quantum yields increased by one order of magnitude upon reaction with the molecular target.
2304 related Products with: Orthogonally Protected Diaminoterephthalate Scaffolds: Installation of Two Functional Units at the Chromophore.Single Strand DNA Ligase, Single Strand DNA Ligase, Thermostable TDG Enzyme & Thermostable TDG Kit Thermostable TDG Kit (DIS Thermostable TDG Kit *DIS Includes 10 X reaction bu Includes 10 X reaction bu Twort's Counterstain Kit ATF3 RNase H (E. coli), recomb RNase H (E. coli), recomb
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Covalently mucoadhesive amphiphilic prodrug of 5-fluorouracil for enhanced permeation and improved oral absorption.5-Fluorouracil (5-FU) is one of the important antitumor drugs and is widely used to treat various types of cancers. However, its administration is limited to intravenous route due to poor oral bioavailability. Herein, we hypothesized that the maleimide group-containing 5-FU prodrug (EMC-5-FU) could improve the intestinal mucoadhesion because the maleimide end group can covalently target thiol residues of mucin glycoprotein covering the intestinal enterocytes. In vitro bioadhesion results showed that EMC-5-FU exhibited good affinity to the cysteine-rich subdomains of mucin and NMR studies successfully verified the covalent attachment of EMC-5-FU to mucin. The intestinal perfusion study indicated that the intestinal bioadhesion and membrane permeability are greatly enhanced for EMC-5-FU, in comparison with 5-FU. Mucoadhesion investigations on rat intestine intuitively confirmed increased intestinal retention of 5-FU through maleimide-mediated mucoadhesion. Moreover, AUCof the total 5-FU level for EMC-5-FU solution was 2.65-fold higher compared with 5-FU solution. Our study further suggested that the amphiphilic prodrug EMC-5-FU with good mucoadhesion is a promising delivery strategy form to overcome multiple barriers of oral absorption.
2712 related Products with: Covalently mucoadhesive amphiphilic prodrug of 5-fluorouracil for enhanced permeation and improved oral absorption.Cellufine Formyl , 50 ml Cellufine Formyl Media Cellufine Formyl , 500 ml Cellufine Formyl Media Cellufine Formyl Media Formalin Solution (20%) Formalin Solution (20%) Formalin Solution (20%) Formalin (10% Neutral Bu Formalin (10% Neutral Bu Nuclear Fast Red Solutio Nuclear Fast Red Solutio
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Chemical cleavage of Asp-Cys sequence allows efficient production of recombinant peptides with an N-terminal cysteine residue.Peptides with an N-terminal cysteine residue allow site-specific modification of proteins and peptides and chemical synthesis of proteins. They have been widely used to develop new strategies for imaging, drug discovery, diagnostics and chip technologies. Here we present a method to produce recombinant peptides with an N-terminal cysteine residue as a convenient alternative to chemical synthesis. The method is based on the release of the desired peptide from a recombinant fusion protein by mild acid hydrolysis of an Asp-Cys sequence. To test the general validity of the method we prepared four fusion proteins bearing three different peptides (20-37 amino acid long) at the C-terminus of a ketosteroid isomerase-derived and two Onconase-derived carriers for the production of toxic peptides in E. coli. The chosen peptides were (C)GKY20, an antimicrobial peptide from the C-terminus of human thrombin, (C)ApoBL,, an antimicrobial peptide from an inner region of human Apolipoprotein B, and (C)p53pAnt, an anticancer peptide containing the C-terminal region of the p53 protein fused to the cell penetrating peptide Penetratin. Cleavage efficiency of Asp-Cys bonds in the four fusion proteins was studied as function of pH, temperature and incubation time. In spite of the differences in the amino acid sequence (GTGDCGKY, GTGDCHVA, GSGTDCGSR, SQGSDCGSR) we obtained for all the proteins a cleavage efficiency of about 70-80% after 24 h incubation at 60°C and pH 2. All the peptides were produced with very good yield (5-16 mg/L of LB cultures), high purity (>96%) and the expected content of free thiol groups (1 mole per mole of peptide). Furthermore, (C)GKY20 was modified with PyMPO-maleimide, a commercially available fluorophore bearing a thiol reactive group, and with 6-hydroxy-2-cyanobenzothiazole, a reagent specific for N-terminal cysteines, with yields of 100% thus demonstrating that our method is very well suited for the production of fully reactive peptides with an N-terminal cysteine residue.
2457 related Products with: Chemical cleavage of Asp-Cys sequence allows efficient production of recombinant peptides with an N-terminal cysteine residue.D Cysteine hydrochloride L Cysteine hydrochloride L Cysteine hydrochloride Rat monoclonal anti mouse Anti-Conjugated D-Cystein HIV 1 tat recombinant ant HIV 1 gag p24 recombinant HIV 1 nef recombinant ant HIV 1 env gp41 recombinan HIV 2 env gp36 recombinan HCV core recombinant anti HCV core recombinant anti
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Insights into maleimide - thiol conjugation chemistry: conditions for efficient surface functionalization of nanoparticles for receptor targeting.Maleimide-thiol chemistry is widely used for the design and preparation of ligand-decorated drug delivery systems such as poly(lactide-co-glycolide) (PLGA) based nanoparticles (NPs). While many publications on nanocarriers functionalized exploiting this strategy are available in the literature, the conditions at which this reaction takes place vary among publications. This paper presents a comprehensive study on the conjugation of the peptide cRGDfK and the nanobody 11A4 (both containing a free thiol group) to maleimide functionalized PLGA NPs by means of the maleimide-thiol click reaction. The influence of different parameters, such as the nanoparticles preparation method and storage conditions as well as the molar ratio of maleimide to ligand used for conjugation, on the reaction efficiency has been evaluated. The NPs were prepared by a single or double emulsion method using different types and concentrations of surfactants and stored at 4 or 20 °C before reaction with the targeting moieties. Several maleimide to ligand molar ratios and different reaction times were studied and the conjugation efficiency was determined by quantification of the not-bound ligand by liquid chromatography. The kind of emulsion used to prepare the NPs as well as the type and concentration of surfactant used had no effect on the conjugation efficiency. Reaction between the maleimide groups present in the NPs and cRGDfK was optimal at a maleimide to thiol molar ratio of 2:1, reaching a conjugation efficiency of 84 ± 4% after 30 min at room temperature in 10 mM HEPES pH 7.0. For 11A4 nanobody the optimal reaction efficiency, 58 ± 12%, was achieved after 2 h of incubation at room temperature in PBS pH 7.4 using a 5:1 maleimide to protein molar ratio. Storage of the NPs at 4 °C for 7 days prior to their exposure to the ligands resulted in approximately 10% decrease in the reactivity of maleimide in contrast to storage at 20 °C which led to almost 40% of the maleimide being unreactive after the same storage time. Our findings demonstrate that optimization of this reaction, particularly in terms of reactant ratios, can represent a significant increase in the conjugation efficiency and prevent considerable waste of resources.
1192 related Products with: Insights into maleimide - thiol conjugation chemistry: conditions for efficient surface functionalization of nanoparticles for receptor targeting.Cellufine Formyl , 50 ml Cellufine Formyl Media Cellufine Formyl , 500 ml Cellufine Formyl Media Cellufine Formyl Media Formalin Solution (20%) Formalin Solution (20%) Formalin Solution (20%) Formalin (10% Neutral Bu Formalin (10% Neutral Bu Zinc Formalin Solution Zinc Formalin Solution
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Fast, irreversible modification of cysteines through strain releasing conjugate additions of cyclopropenyl ketones.A method of cysteine alkylation using cyclopropenyl ketones is described. Due to the significant release of cyclopropene strain energy, reactions of thiols with cyclopropenyl ketones are both fast and irreversible and give rise to stable conjugate addition adducts. The resulting cyclopropenyl ketones have a low molecular weight and allow for simple attachment of amides via N-hydroxysuccinimide (NHS)-esters. While cyclopropenyl ketones do display slow background reactivity toward water, labeling by thiols is much more rapid. The reaction of a cyclopropenyl ketone with glutathione (GSH) proceeds with a rate of 595 Msin PBS at pH 7.4, which is considerably faster than α-halocarbonyl labeling reagents, and competitive with maleimide/thiol couplings. The method has been demonstrated in protein conjugation, and an arylthiolate conjugate was shown to be stable upon prolonged incubation in either GSH or human plasma. Finally, cyclopropenyl ketones were used to create PEG-based hydrogels that are stable to prolonged incubation in a reducing environment.
2727 related Products with: Fast, irreversible modification of cysteines through strain releasing conjugate additions of cyclopropenyl ketones.Ofloxacin CAS Number [824 Cell Strainers 40μm Cell Cell Strainers 70μm Cell Cell Strainers 100μm Cel SensiTek Alk-Phos Anti-M SensiTek Alk-Phos Anti-R SensiTek Alk-Phos Anti-P UltraTek Alk-Phos Anti-M EconTek Alk-Phos Anti-Po UltraTek Alk-Phos Anti-R UltraTek Alk-Phos Anti-P Acid Fast Bacteria (AFB)
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