Enoximone is a phosphodiesterase 3 (PDE3) inhibitor (IC50 = 5.9 µM).{56134} It is selective for PDE3 over PDE1, -2, and -4 (IC50s = 2,100, 2,900, and 21.1 µM, respectively). Enoximone increases the force of contraction and cAMP levels in isolated canine right ventricular trabeculae, an effect that can be reversed by carbamoylcholine (carbachol; Item No. 14486).{56135} In vivo, enoximone (0.1-1 mg/kg) increases cardiac contractile force in dogs.{56136} Formulations containing enoximone have been used in the treatment of congestive heart failure.
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A PDE3 inhibitor (IC50 = 5.9 µM); selective for PDE3 over PDE1, -2, and -4 (IC50s = 2,100, 2,900, and 21.1 µM, respectively); increases the force of contraction and cAMP levels in isolated canine right ventricular trabeculae; increases cardiac contractile force in dogs from 0.1-1 mg/kg
Formal name: 1,3-dihydro-4-methyl-5-[4-(methylthio)benzoyl]-2H-imidazol-2-one
Synonyms: MDL 17043
Molecular weight: 248.3
CAS: 77671-31-9
Purity: ≥98%
Formulation: A solid
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 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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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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