PSB-KD107 is an agonist of the orphan G protein-coupled receptor GPR18 (EC50 = 0.56 µM in a β-arrestin recruitment assay using CHO cells expressing the human receptor).{58090,44024} It is selective for GPR18 over GPR55, as well as cannabinoid (CB) receptor 1 (CB1) and CB2, at 10 µM but also binds to the adenosine A2A receptor (Ki = 0.33 µM for the rat receptor).{58090,58091}
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A GPR18 agonist (EC50 = 0.56 µM in a β-arrestin recruitment assay using CHO cells expressing the human receptor); selective for GPR18 over GPR55, as well as CB1 and CB2, at 10 µM but also binds to the adenosine A2A receptor (Ki = 0.33 µM for the rat receptor)
Formal name: 6,7,8,9-tetrahydro-9-[2-(1H-indol-3-yl)ethyl]-1,3-dimethyl-pyrimido[2,1-f]purine-2,4(1H,3H)-dione
Synonyms:
Molecular weight: 378.4
CAS: 955121-65-0
Purity: ≥98%
Formulation: A crystalline 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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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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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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