Diosmetin-d3 is intended for use as an internal standard for the quantification of diosmetin (Item No. 18649) by GC- or LC-MS. Diosmetin is a flavonoid that has been found in citrus fruits and has diverse biological activities.{30253,49507,49508,49509} It inhibits the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1B1 (Kis = 89 and 16 nM, respectively).{30253} Diosmetin prevents increases in erythrocyte reactive oxygen species (ROS) and malondialdehyde (MDA) levels induced by AAPH (Item No. 82235) in a concentration-dependent manner.{49507} It reduces tumor growth and tumor blood vessel density in a B16/F10 murine melanoma model when administered at a dose of 1 mg/kg twice per day.{49508} Diosmetin (0.5 mg/kg) inhibits lung goblet cell hyperplasia and collagen deposition and decreases the number of eosinophils and neutrophils in bronchoalveolar lavage fluid (BALF) in a mouse model of chronic asthma induced by ovalbumin.{49509}
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An internal standard for the quantification of diosmetin by GC- or LC-MS
Formal name: 5,7-dihydroxy-2-(3-hydroxy-4-methoxy-d3-phenyl)-4H-1-benzopyran-4-one
Synonyms: Diosmetol-d3|Luteolin 4′-methyl ester-d3
Molecular weight: 303.3
CAS: 1189728-54-8
Purity: ≥99% deuterated forms (d1-d3)
Formulation: A solid
The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
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The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
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The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}
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