5-Butyl-4-[2,3-difluoro-4-(phenylmethoxy)phenyl]-6-phenyl-2-pyrimidinamine is an inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1; IC50s = 66 and 2,730 nM for the human and mouse enzymes, respectively).{52747} It is selective for mPGES-1 over COX-1 but does inhibit COX-2 at 20 µM. It also inhibits LPS-induced prostaglandin E2 (PGE2; Item No. 14010) production in mouse peritoneal cells (IC50 = 12 nM). In vivo, 5-butyl-4-[2,3-difluoro-4-(phenylmethoxy)phenyl]-6-phenyl-2-pyrimidinamine (25 mg/kg) reduces carrageenan-induced paw edema in rats.
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An mPGES-1 inhibitor (IC50s = 66 and 2,730 nM for human and mouse enzymes, respectively); selective for mPGES-1 over COX-1 but does inhibit COX-2 at 20 µM; inhibits LPS-induced PGE2 production in mouse peritoneal cells (IC50 = 12 nM); reduces carrageenan-induced paw edema in rats at 25 mg/kg
Formal name:
Synonyms:
Molecular weight: 445.5
CAS: 2253745-78-5
Purity: ≥98%
Formulation: A solution in methyl acetate
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 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 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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