2-Nonylquinolin-4(1H)-one is a quinolone alkaloid that has been found in P. aeruginosa and has diverse biological activities.{58183,58184,58185,58188} It reduces infection of Huh7.5 cells by hepatitis C virus (HCV) with an IC50 value of 1.4 µg/ml.{58183} 2-Nonylquinolin-4(1H)-one (50 and 100 µg/ml) is also active against L. gongylophorus, a symbiotic fungus of the agricultural pest A. sexdens (leaf-cutting ant).{58184} It inhibits activation of nuclear factor of activated T cells (NFAT) induced by phorbol 12-myristate 13-acetate (TPA; Item No. 10008014) and the calcium ionophore A23187 (Item No. 11016) in Jurkat cells (IC50 = 3.44 µM), but not LPS-induced NF-κB activation in RAW 264.7 cells (IC50 = >100 µM), in reporter assays.{58185} This compound is expected to exist in one or both tautomeric forms, depending on experimental conditions.
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A quinolone alkaloid; active against HCV (IC50 = 1.4 µg/ml) and L. gongylophorus; inhibits TPA- and A23187-induced NFAT activation in Jurkat cells but not LPS-induced NF-κB activation in RAW 264.7 cells (IC50s = 3.44 and >100 µM, respectively, in reporter assays)
Formal name:
Synonyms: 2-n-Nonyl-4-quinolone|2-Nonyl-1H-quinolin-4-one|2-Nonylquinolin-4(1H)-one|Pseudane IX
Molecular weight: 271.4
CAS: 55396-45-7
Purity: ≥95%
Formulation: A crystalline solid
Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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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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Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
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