Arachidonoyl ethanolamide (AEA, Item No. 90050), also known as anandamide, is an endogenous ligand of the cannabinoid receptors.{2713} AEA is metabolized by fatty acid amide hydrolase (FAAH) to give arachidonic acid (Item No. 90010) and ethanolamine.{15373} ARN1203 is a fluorinated analog of AEA that serves as a substrate of FAAH (Km = 29 µM).{25931} Fluorinated substrates, like ARN1023, are used in ‘n-fluorine atoms for biochemical screening’ (n-FABS) assays, NMR functional assays that directly measure the conversion of the substrate into product.{25932} ARN1203 is used to perform n-FABS against FAAH to identify novel inhibitors.{25931, 25932,25933}
A fluorinated analog of AEA that serves as a substrate of FAAH (Km = 29 µM); used to perform n-FABS against FAAH to identify novel inhibitors
Formal name: N-(3-fluoro-2-hydroxypropyl)-5Z,8Z,11Z,14Z-eicosatetraenamide
Synonyms:
Molecular weight: 379.6
CAS: 1428445-15-1
Purity: ≥98%
Formulation: A solution in ethanol
Product Type|Biochemicals|Labeling & Detection|Enzyme Substrates||Product Type|Biochemicals|Labeling & Detection|Fluorescent Probes||Research Area|Lipid Biochemistry
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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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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