Prostaglandin E1 isopropyl ester is an ester prodrug form of prostaglandin E1 (PGE1; Item No. 13010) with enhanced lipid solubility.{49642,49641} The ester functional group on PGE1 isopropyl ester is readily hydrolyzed in cells and in vivo to release active PGE1.{49642} PGE1 isopropyl ester exhibits a faster penetration flux than the free acid form of PGE1 when applied topically to isolated mouse skin. Topical administration of PGE1 isopropyl ester (1 mM) reduces fluid pressure within human dermal fibroblast cell aggregates.{49641}
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An ester prodrug form of PGE1; exhibits a faster penetration flux than the free acid form of PGE1 when applied topically to isolated mouse skin; topical administration reduces fluid pressure within human dermal fibroblast cell aggregates at 1 mM,,
Formal name: (11α,13E,15S)-11,15-dihydroxy-9-oxo-prost-13-en-1-oic acid, 1-methylethyl ester
Synonyms: PGE1 isopropyl ester
Molecular weight: 396.6
CAS: 217182-28-0
Purity: ≥95%
Formulation: A solution methyl acetate
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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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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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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