rPLA2 is a calcium-dependent cytosolic phospholipase A2 (cPLA2) initially isolated and characterized from bovine and human red blood cells (RBCs).{10767} It has a molecular mass of 42 kDa and biochemical properties similar to cPLA2 Type IV. EA4 is a quinone derivative that inhibits rPLA2 with a Ki of 130 µM. It inhibits the ionophore-induced arachidonic acid release from human and bovine red blood cells (RBCs), indicating that rPLA2 is responsible for the Ca2+-dependent release of arachidonic acid from mammalian RBCs.{10767} EA4 causes significant time- and concentration-dependent induction of cytochrome P450 1A1 (CYP1A1) mRNA and protein in murine hepatoma Hepa-1c1c7 cells.{13350} EA4 also modulates CYP1A1 and CYP1B1 expression in other cell lines such as MCF-7, Hep-G2, and HL-60.{13350}
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A quinone derivative that inhibits red blood cell PLA2 with a Ki value of 130 µM
Formal name: 7-chloro-6-[4-(diethylamino)phenyl]-5,8-quinolinedione
Synonyms:
Molecular weight: 340.8
CAS: 389614-94-2
Purity: ≥95%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors|Phospholipases||Research Area|Lipid Biochemistry|Glycerophospholipids|Phospholipases||Research Area|Toxicology|Drug Metabolism|Cytochrome P450
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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The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.
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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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