Category: 130345-50-5

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Phosphoinositol 3-kinase-gamma mediates antineutrophil cytoplasmic autoantibody-induced glomerulonephritis

Antineutrophil cytoplasmic autoantibodies (ANCA) are associated with necrotizing crescentic glomerulonephritis (NCGN) and systemic vasculitis. We examined the role of phosphoinositol 3 kinase-gamma isoform (PI3Kgamma) in ANCA-activated neutrophil functions. Further, we tested whether its inhibition protects a mouse model of ANCA NCGN from developing NCGN. We transplanted bone marrow from wild-type mice or PI3Kgamma-deficient mice into myeloperoxidase-deficient mice immunized with myeloperoxidase. Bone marrow from PI3Kgamma / mice protected against development of the disease. Similarly, bone marrow transplanted from wild-type mice followed by treatment with the specific PI3Kgamma inhibitor AS605240 also protected these mice against NCGN in this model. AS605240 significantly abrogated myeloperoxidase-or proteinase 3-ANCA-stimulated superoxide production in vitro. Furthermore, ANCA-induced degranulation and GM-CSF-stimulated migration in a transwell assay of isolated human neutrophils were also abrogated by the drug. We found that PI3Kgamma plays a pivotal role in ANCA-induced NCGN and suggest that its specific inhibition may provide a novel treatment target.

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Reference：
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N230 | ChemSpider

Application of 130345-50-5, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.130345-50-5, Name is Quinoxaline-6-carbaldehyde, molecular formula is C9H6N2O. In a article，once mentioned of 130345-50-5

6-O-acyl ketolide antibacterials

6-O-Acyl ketolide antibacterials of the formula: 1wherein R1, R2, R3, R4, W, X, X?, Y, and Y? are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N199 | ChemSpider

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Activity of novel quinoxaline-derived chalcones on in vitro glioma cell proliferation

Gliomas are the most common and devastating tumors of the central nervous system (CNS). Many pieces of evidence point out the relevance of natural compounds for cancer therapy and prevention, including chalcones. In the present study, eight synthetic quinoxaline-derived chalcones, structurally based on the selective PI3Kgamma inhibitor AS605240, were evaluated for anti-proliferative activity and viability inhibition using glioma cell lines from human and rat origin (U-138 MG and C6, respectively), at different time-periods of incubation and concentrations. The results revealed that four chalcones (compounds 1, 6, 7 and 8), which present methoxy groups at A-ring, displayed higher efficacies and potencies, being able to inhibit either cell proliferation or viability, in a time- and concentration-dependent manner, with an efficacy that was greater than that seen for the positive control compound AS605240. Flow cytometry analysis demonstrated that incubation of C6 cells with compound 6 led to G1 phase arrest, likely indicating an interference with apoptosis. Furthermore, compound 6 was able to visibly inhibit AKT activation, allied to the stimulation of ERK MAP-kinase. The chalcones tested herein, especially those displaying a methoxy substituent, might well represent promising molecules for the adjuvant treatment of glioma progression.

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Reference：
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N226 | ChemSpider

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: Quinoxaline-6-carbaldehyde, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 130345-50-5, name is Quinoxaline-6-carbaldehyde. In an article，Which mentioned a new discovery about 130345-50-5

A series of novel derivatives of the nonsteroidal anti-inflammatory drug (NSAID) sulindac sulfide were synthesized as potential agonists of the peroxisome proliferator-activated receptor gamma (PPARgamma). Nonpolar and aromatic substitutions on the benzylidene ring as well as retention of the carboxylic acid side chain were required for optimal activity. Compound 24 was as potent a compound as any other in the series with an EC50 of 0.1 muM for the induction of peroxisome proliferator response element (PPRE)-luciferase activity. Direct binding of compound 24 to PPARgamma was demonstrated by the displacement of [3H]troglitazone, a PPARgamma agonist, in a scintillation proximity assay. Compound 24 also stimulated the binding of PPARgamma to a PPRE-containing oligonucleotide and induced expression of liver fatty-acid binding protein (L-FABP) and adipocyte fatty acid-binding protein (aP2), two established PPARgamma target genes. Taken together, these compounds represent potential leads in the development of novel PPARgamma agonists.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N223 | ChemSpider

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BICYCLIC OGA INHIBITOR COMPOUNDS

The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer’s disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations.

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Reference：
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N205 | ChemSpider

Synthetic Route of 130345-50-5, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 130345-50-5, Name is Quinoxaline-6-carbaldehyde, molecular formula is C9H6N2O. In a Patent，once mentioned of 130345-50-5

NOVEL CHEMICAL COMPOUNDS

This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N216 | ChemSpider

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PIPERAZINYLIMIDAZOPYRIDINE AND PIPERAZINYLTRIAZOLOPYRIDINE ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE RECEPTOR

The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists.

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Reference：
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N218 | ChemSpider

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CERTAIN CHEMICAL ENTITES, COMPOSITIONS, AND METHODS

Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N211 | ChemSpider

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Method for preparing heterocyclic-carboxylic acids

The present invention relates to a method for preparing quinoxaline-5- and 6-carboxylic acids. The method comprises contacting an aqueous suspension of a 5- or 6-hydroxymethyl quinoxaline with oxygen in the presence of a transition metal catalyst, to form the respective quinoxaline-5- or 6-carboxylic acid. The method for oxidizing benzylic methyl groups may also be employed to prepare a wide variety of heterocyclic carboxylic acid compounds.

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Reference£º
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N195 | ChemSpider

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A new family of quinoline and quinoxaline analogues of combretastatins

The 3-hydroxy-4-methoxyphenyl ring of combretastatin A-4 can be replaced by a 2-naphthyl moiety without significant loss of cytotoxicity and inhibition of tubulin polymerization potency. In this paper we show that the 6- or 7-quinolyl systems can in turn replace both cyclic moieties, keeping in the first case most of the potency as cytotoxic agent and in the second case as inhibitor of tubulin polymerization, related to the activities displayed by model compounds.

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Reference£º
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N228 | ChemSpider