U-51605 is a stable analog of the endoperoxide prostaglandin H2 (PGH2). It is an inhibitor of both prostacyclin (PGI) and thromboxane (TX) synthases with more selectivity towards PGI synthase. U-51605 is also a partial agonist at TP receptors.{817} In human foreskin fibroblasts, U-51605 inhibits PGI synthase at a concentration of 2.8 µM, whereas, human platelet TX synthase is inhibited at a concentration of 5.6 µM.{818,486} At concentrations up to 1 µM, U-51605 reduced the release of prostacyclin in SHR aorta elicited by the calcium ionophore A-23187 with no effect on TXA2 production and yet significantly increased PGE2 and PGF2α release.{18479}
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A stable analog of PGH2 that inhibits both PGI and TX synthases with more selectivity towards PGI synthase; a partial agonist at TP receptors
Formal name: 9α,11α-azoprosta-5Z,13E-dien-1-oic acid
Synonyms:
Molecular weight: 332.5
CAS: 64192-56-9
Purity: ≥98%
Formulation: A solution in methyl acetate
Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Blood||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway
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 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 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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