Zinc pyrithione is a coordination complex of zinc and pyrithione that has antimicrobial and anticancer activities.{47777,47778,47779} It is active against the bacteria E. coli, S. aureus, K. pneumoniae, A. baumannii, P. aeruginosa, E. faecium, E. faecalis, and E. cloacae (MICs = 1-4 µg/ml) and the fungus P. ovale when used at concentrations ranging from 0.01 to 10 µg/ml.{47777,47778} Zinc pyrithione reduces tumor growth in an SCC-4 mouse xenograft model when administered at a dose of 1 mg/kg per week for six weeks.{47779} Formulations containing zinc pyrithione have been used in the treatment of dandruff.
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A coordination complex of zinc and pyrithione that has antimicrobial and anticancer activities; active against various bacteria (MICs = 1-4 µg/ml) and the fungus P. ovale at 0.01-10 µg/ml; reduces tumor growth in an SCC-4 mouse xenograft model at 1 mg/kg per week for six weeks
Formal name: (T-4)-bis[1-(hydroxy-κO)-2(1H)-pyridinethionato-κS2]-zinc
Synonyms:
Molecular weight: 317.7
CAS: 13463-41-7
Purity: ≥95%
Formulation: A solid
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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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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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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