Tag: M.W=400-500

Application of 70539-42-3. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, is researched, Molecular C18H20N2O12, CAS is 70539-42-3, about Modulation of two forms of tumor necrosis factor receptors and their cellular response by soluble receptors and their monoclonal antibodies. Author is Higuchi, Masahiro; Aggarwal, Bharat B..

Recently, two different receptors for human tumor necrosis factor (TNF) with mol. masses of 60 kDa (p60) and 80 kDa (p80) have been identified. This report investigated the effect of the soluble forms of these receptors and monoclonal antibodies against them on ligand interaction, receptor down-regulation, and mediation of cellular response in U-937 cells. The results indicate that p60 and p80 constitute 20-30 and 60-80% of the total TNF-binding sites on U-937 cells, resp. However, by crosslinking, only the p80 form of the receptor could be detected. In contrast to unlabeled TNF, the anti-p60 and anti-p80 antibodies together only partially inhibited ligand binding, and this inhibition was not additive. Lack of additive inhibition of binding was not due to stereochem. hindrance. TNF binding to cells can be completely displaced by soluble forms of either the p60 or p80 receptor. However, 100-fold more of the p80 than the p60 form of the soluble receptor is needed for equivalent displacement. Under optimum conditions, TNF and the anti-p80 and anti-p60 antibodies down-regulated 30, 80, and 20% of the TNF receptors, resp. The anti-p60 and anti-p80 antibodies down-regulated not only their own receptors, but also reciprocal receptors, suggesting a cross-communication between the p60 and p80 forms of the TNF receptor. In spite of inhibiting as much as 80% of TNF binding, none of the receptor antibodies significantly inhibited the cytotoxic response to TNF in U-937 cells. Soluble forms of both receptors, however, completely abrogated the cellular response to TNF. Thus, these results indicate that the antibodies against both receptors together inhibit the majority of the receptor-ligand interaction without any significant effect on the biol. response to TNF.

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Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Shi, An-Guo; Deth, Richard C. researched the compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate( cas:70539-42-3 ).Formula: C18H20N2O12.They published the article 《Precoupling of alpha-2B adrenergic receptors and G-proteins in transfected PC-12 cell membranes: influence of pertussis toxin and a lysine-directed cross-linker》 about this compound( cas:70539-42-3 ) in Journal of Pharmacology and Experimental Therapeutics. Keywords: alpha2B adrenergic receptor precoupling G protein. We’ll tell you more about this compound (cas:70539-42-3).

The ability of pertussis toxin (PTX) pretreatment to alter the binding of [3H]rauwolscine (RAU) to alpha-2B adrenergic receptors expressed in PC12 cells was examined PTX caused a 30% increase in the Bmax for [3H]RAU and reduced its KD, whereas in the added presence of Na+ and Gpp(NH)p binding was increased to 75% above the level in untreated membranes. Because all three agents act to reduce receptor/G-protein affinity, the increased binding may reflect extensive precoupling of the alpha-2B receptor. The affinity of the agonist epinephrine in displacing [3H]RAU was normally reduced by both Na+ and Gpp(NH)p; however, in PTX-treated membranes the effect of Gpp(NH)p was eliminated, and Na+ remained effective. The lysine-directed crosslinking reagent ethyleneglycol bis(succinimidyl)succinate (EGS) was utilized to cross-link precoupled receptor and G-protein. Maximal [3H]RAU binding was reduced by EGS in a time- and dose-dependent manner, and this action was reversed by prior incubation with Na+ and Gpp(NH)p, suggesting that EGS did indeed cross-link receptor and G-protein. RAU and epinephrine each provided protection against the effect of EGS. The inclusion of Na+ and Gpp(NH)p during [3H]RAU binding studies was able to restore maximal binding in EGS-treated membranes to the same level as untreated membranes. These results indicate that in the absence of Na+ and Gpp(NH)p at least 40% of the total alpha-2B adrenergic receptors in these membranes exist as a precoupled receptor/G-protein complex which fails to bind [3H]RAU.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Identification of peptide fragments chemically cross-linked in cytochrome c oxidase from thermophilic Bacillus PS3, published in 1996-02-29, which mentions a compound: 70539-42-3, mainly applied to Bacillus cytochrome c oxidase structure crosslinking; protein quaternary domain structure crosslinking method, Category: benzofurans.

In order to study steric arrangement of subunits in cytochrome c oxidase isolated from thermophilic Bacillus PS3, we developed a simple procedure including chem. crosslinking, two consecutive runs of electrophoresis, proteolytic digestion, and peptide sequencing for simultaneous identification of two cross-linked fragments. By this procedure, the cytochrome c domain of subunit 2 was found cross-linked to the C-terminal region of subunit 1 including two hydrophobic transmembrane segments, suggesting that these two regions were located close each other. The present simple procedure might be applicable to proteins whose crystal structures are not revealed.

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Benzofuran – Wikipedia,
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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, is researched, Molecular C18H20N2O12, CAS is 70539-42-3, about Covalent coupling of bovine growth hormone to its receptor in bovine liver membranes, the main research direction is somatotropin receptor liver membrane cattle.SDS of cas: 70539-42-3.

The structure of bovine somatotropin receptor was examined following covalent coupling of iodinated recombinant bovine growth hormone ([125I]rbGH) to bovine liver membrane receptors using ethylene glycol bis(succinimidyl succinate). Iodinated rbGH was incorporated into a complex of estimated mol. weight (Mr) of 140,000 under reducing conditions. Excess unlabeled rbGH, but not bovine prolactin (bPRL), inhibited completely the incorporation of [125I]rbGH into the Mr = 140,000 species. In dairy bulls, the Mr = 140,000 complex was undetectable soon after birth but became predominant at 6 mo of age. No evidence was found to support presence of bPRL receptors in steer liver membranes. Assuming a 1:1 stoichiometry of hormone binding to receptor, it appears that bGH binds to a major receptor subunit of Mr = 119,000 which does not recognize bPRL.

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Benzofuran – Wikipedia,
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Related Products of 70539-42-3. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, is researched, Molecular C18H20N2O12, CAS is 70539-42-3, about Characterization and affinity cross-linking of receptors for human recombinant lymphotoxin (tumor necrosis factor-β) on a human histiocytic lymphoma cell line, U-937. Author is Stauber, Gregory B.; Aggarwal, Bharat B..

Recombinant human lymphotoxin (rhLT) was purified and used to examine its receptors on the human histiocytic lymphoma cell line U-937. The rhLT was radioiodinated by the IODO GEN method to a specific activity of 60 μCi/μg. The specific binding reached a plateau within 10, 60, and 180 min at 37, 23, and 4°, resp. Scatchard anal. revealed the presence of a single class of high affinity receptors with an apparent Kd of 0.6 nm and a capacity of 33,000 binding sites/cell. The binding of 125I-labeled rhLT to U-937 cells was inhibited by excess unlabeled rhLT or recombinant human tumor necrosis factor-α(rhTNF), suggesting a common receptor for both mols. The crosslinking of the receptor to rhLT revealed 2 distinct bands at approx. mol. masses of 100,000 and 120,000 daltons. Affinity crosslinking of U-937 cells with 125I-labeled rhTNF, however, provided only a single band with a mol. mass of about 100,000 daltons. Thus, the manner in which rhLT interacts with its receptor is perhaps somewhat different from that of rhTNF.

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Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, is researched, Molecular C18H20N2O12, CAS is 70539-42-3, about Chemically stabilized trypsin used in dipeptide synthesis, the main research direction is trypsin chem stabilized preparation dipeptide synthesis; benzoylarginylleucinamide synthesis higher yield modified trypsin.HPLC of Formula: 70539-42-3.

Bovine pancreatic trypsin was treated with ethylene glycol bis(succinic acid N-hydroxysuccinimide ester), such that approx. 8 out of 14 lysines per trypsin mol. were modified. This derivative (EG trypsin) was more stable than native between 30° and 70°: T50 values were 59° and 46°, resp. EG trypsin’s half-life of 25 min at 55° was fivefold greater than native’s. EG trypsin had a decreased rate of autolysis and retained more activity in aqueous mixtures of 1,4-dioxan, DMF, dimethylsulfoxide, and acetonitrile. EG trypsin had lower Km values for both amide and ester substrates; its kcat values for two amides (PhCO-Arg-NHC6H4NO2-4 and Cbz-Gly-Gly-Arg-NMC; NMC = 7-amino-4-methylcoumarin) increased, whereas its kcat value for an ester (Cbz-Lys-SCOPh) decreased slightly. The specific activity (kcat/Km) of EG trypsin was increased for both amide and ester substrates. EG trypsin gave higher yields and reaction rates than the native trypsin in kinetically controlled synthesis of PhCO-Arg-Leu-NH2 in acetonitrile and in t-butanol. Highest peptide yields occurred with EG trypsin in 95% acetonitrile, where 90% of the substrate was converted to product. No peptide synthesis occurred in 95% DMF with either form of trypsin.

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Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Recommanded Product: 70539-42-3. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, is researched, Molecular C18H20N2O12, CAS is 70539-42-3, about Analysis of the molecular organization of recombinant human tumor necrosis factor (rTNF) in solution using ethylene glycolbis(succinimidylsuccinate) as the cross-linking reagent. Author is Lam, Kit S.; Scuderi, Philip; Salmon, Sydney E..

Anal. of chem. cross-linked recombinant human tumor necrosis factor (rTNF) on SDS-PAGE revealed the presence of 3 distinct mol. forms which correspond to trimers, dimers, and monomers. The crosslinking procedure appeared to enhance the antigenicity of these mol. forms of rTNF as determined by Western blot anal. Crosslinking was unaffected by 2% Nonidet P-40, high concentrations of human serum albumin, or 60% normal human serum. SDS (0.08%) completely abolished the crosslinking of rTNF. The rTNF, at a concentration as low as 0.8 ng/mL, exists solely in the trimeric form in solution under nondenaturing conditions.

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Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Reference of Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, is researched, Molecular C18H20N2O12, CAS is 70539-42-3, about Polyaspartamide-Doxorubicin Conjugate as Potential Prodrug for Anticancer Therapy. Author is Di Meo, Chiara; Cilurzo, Felisa; Licciardi, Mariano; Scialabba, Cinzia; Sabia, Rocchina; Paolino, Donatella; Capitani, Donatella; Fresta, Massimo; Giammona, Gaetano; Villani, Claudio; Matricardi, Pietro.

The purpose of this study was to synthesize a new polymeric prodrug based on α,β-poly(N-2-hydroxyethyl)(2-aminoethylcarbamate)-d,l-aspartamide copolymer bearing amine groups in the side chain (PHEA-EDA), covalently linked to the anticancer drug doxorubicin and to test its potential application in anticancer therapy. The drug was previously derivatized with a biocompatible and hydrophilic linker, leading to a doxorubicin derivative highly reactive with amino groups of PHEA-EDA. The PHEA-EDA-DOXO prodrug was characterized in terms of chem. stability. The pharmacokinetics, biodistribution and cytotoxicity of the product was investigated in vitro and in vivo on human breast cancer MCF-7 and T47D cell lines and NOD-SCID mice bearing a MCF-7 human breast carcinoma xenograft. Data collected were compared to those obtained using free doxorubicin. The final polymeric product is water soluble and easily hydrolysable in vivo, due to the presence of ester and amide bonds along the spacer between the drug and the polymeric backbone. In vitro tests showed a retarded cytotoxic effect on tumor cells, whereas a significant improvement of the in vivo antitumor activity of PHEA-EDA-DOXO and a survival advantage of the treated NOD-SCID mice was evidenced, compared to that of free doxorubicin. The features of the PHEA-EDA-DOXO provide a potential protection of the drug from the plasmatic enzymic degradation and clearance, an improvement of the blood pharmacokinetic parameters and a suitable body biodistribution. The data collected support the promising rationale of the proposed macromol. prodrug PHEA-EDA-DOXO for further potential development and application in the treatment of solid cancer diseases.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Analysis of near-neighbor contacts in bacteriophage T4 wedges and hubless baseplates by using a cleavable chemical cross-linker, published in 1989-06-30, which mentions a compound: 70539-42-3, Name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, Molecular C18H20N2O12, Product Details of 70539-42-3.

Although bacteriophage T4 baseplate morphogenesis has been analyzed in some detail, there is little information available on the spatial arrangement and associations of its 150 subunits. Therefore, anal. of its near-neighbor interactions by using the cleavable chem. cross-linker ethylene glycobis(succinimidylsuccinate) was carried out. The cross-linked complexes that have been identified in the one-sixth arms or wedges and also in baseplatelike structures called rings are described which consist of 6 wedges but lack the central hub, both of which are purified from T4 gene 5–infected cells. Thirty different complexes were identified, of which about half contain multimers of a single species and half contain 2 different species. In general, the complexes reflect and support the assembly pathway derived by Y. Kikuchi and J. King (1975 ), but broaden its scope to include such complexes as gp25-gp53, gp25-gp48, and gp48-gp53, which locate the gp48 binding site over the inner edge of the ring but outside the central hub. The data also supports the view that wedges are assembled from the outer edge inward toward the central hub. Wedge-wedge contact in rings was mediated primarily by gp12 and gp9, the absence of which dramatically destabilized the ring ↔ wedge equilibrium in favor of wedges. Although no heterologous complexes containing gp9 were identified, gp12 contacts unique to rings were observed with both gp10 and gp11.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, is researched, Molecular C18H20N2O12, CAS is 70539-42-3, about The GCN4 leucine zipper can functionally substitute for the heat shock transcription factor’s trimerization domain.COA of Formula: C18H20N2O12.

The heat shock transcription factor (HSF) is the only known sequence-specific, homotrimeric DNA-binding protein. HSF binds to a DNA recognition site called a heat shock element (HSE), which contains varying numbers of nGAAn units (“”GAA boxes””) arranged in inverted repeats. To investigate the role of trimerization on HSF’s DNA-binding properties, the authors replaced the trimerization domain, which self-assembles to form a three-stranded α-helical coiled coil, with the GCN4 leucine zipper, which forms a two-stranded α-helical coiled coil. Surprisingly, this substitution did not effect the ability of HSF to function in vivo. Biochem. studies of an HSF-leucine zipper chimera in comparison to an HSF truncation show that the HSF-leucine zipper chimera, though dimeric in solution and dimeric when bound to a two-box HSE, forms a trimeric complex when bound to a three-box HSE. The ability to form trimers depends on the presence of three contiguous GAA boxes present in inverted repeats. The proximity of the leucine zippers due to the orientation of the binding sites suggests that the leucine zippers might be forming a three-stranded coiled coil and several experiments lend support to this model. The ability of the leucine zipper to change oligomeric states in context might explain why the leucine zipper can replace the trimerization domain of HSF in vivo.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem