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rPLA2 is a calcium-dependent cytosolic phospholipase A2 (cPLA2) initially isolated and characterized from bovine and human red blood cells (RBCs).1 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 RBCs, indicating that rPLA2 is responsible for the Ca2+-dependent release of arachidonic acid from mammalian RBCs.1 EA4 causes significant time- and concentration-dependent induction of cytochrome P450 1A1 (CYP1A1) mRNA and protein in murine hepatoma Hepa-1c1c7 cells.2 EA4 also modulates CYP1A1 and CYP1B1 expression in other cell lines such as MCF-7, Hep-G2, and HL-60.2
1
Shin, H.S., Chin, M., Kim, J.S., et al. Purification and characterization of a cytosolic, 42-kDa and Ca2+-dependent phospholipase A2 from bovine red blood cells. J Biol Chem27721086-21094(2002).
2
Chun, Y.J., Lee, B.Y., Yang, S.A., et al. Induction of cytochrome P450 1A1 gene expression by a vitamin K3 analog in mouse hepatoma Hepa-1c1c7 cells. Mol Cells12190-196(2001).
Room temperature
in continental US; may vary elsewhere
SMILES
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CCN(CC)c1ccc(cc1)C1=C(Cl)C(=O)c2ncccc2C1=O
Background Reading
Shin, H.S., Chin, M., Kim, J.S., et al. Purification and characterization of a cytosolic, 42-kDa and Ca2+-dependent phospholipase A2 from bovine red blood cells. J Biol Chem27721086-21094(2002).
Chun, Y.J., Lee, B.Y., Yang, S.A., et al. Induction of cytochrome P450 1A1 gene expression by a vitamin K3 analog in mouse hepatoma Hepa-1c1c7 cells. Mol Cells12190-196(2001).
EA4 is available in the following screening
library: