Benzodiazepines bind two types of receptors, the central γ-aminobutyric acid A receptor and the peripheral translocator protein (TSPO). PK 11195 binds the peripheral benzodiazepine receptor, TSPO, with selectivity and high affinity (Ki = 3.1 nM in cerebellum, 4.1 nM in spinal cord).{20753,20752} PK 11195, which lacks the 7-member heterocycle of diazepines, blocks binding of typical benzodiazepines to TSPO.{20753} In addition, the binding of labeled PK 11195 to tissues is used to detect the presence of TSPO by various methods.{20752,20751} PK 11195 has been used to study the ligand binding site of the B. cereus TSPO.{28284}
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Binds the peripheral benzodiazepine receptor, TSPO, with selectivity and high affinity (Ki = 3.1 nM in cerebellum, 4.1 nM in spinal cord); blocks binding of typical benzodiazepines to TSPO
Formal name: 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
Synonyms: RP 52028
Molecular weight: 352.9
CAS: 85532-75-8
Purity: ≥98%
Formulation: A solid
Product Type|Biochemicals|Receptor Pharmacology||Research Area|Neuroscience
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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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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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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