Platelet-type 12-lipoxygenase (12-LO; Item No. 10341) catalyzes the formation of 12-HpETE (Item No. 44570) from arachidonic acid (Item No. 90010).{3606} It has been found to be expressed in various tumor cells as well as pancreatic islets and can be activated by inflammatory cytokines.{25127} It has also been implicated in the modulation of hemostasis and thrombosis through its role in regulating platelet function.{25127} CAY10698 is an inhibitor of 12-LO with an IC50 value of 5.1 µM. It demonstrates greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = >50, >40, and >200 µM.{25127} The scaffold of this compound has been subjected to medicinal chemistry optimization and biological characterization for development of potential 12-LO inhibitors.{25127}
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A selective inhibitor of 12-LO with an IC50 value of 5.1 µM
Formal name: 4-[[(2-hydroxy-3-methoxyphenyl)methyl]amino]-N-2-thiazolyl-benzenesulfonamide
Synonyms:
Molecular weight: 391.5
CAS: 684236-01-9
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors|Lipoxygenases||Research Area|Lipid Biochemistry|Lipoxygenase Pathways
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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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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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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