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Product Name:EA4
CAS:389614-94-2
Purity:95% Package:1G;10G;100G Remarks:EA4 is a rPLA2 inhibitor, and it is a quinone derivative. rPLA2, a calcium-dependent cytosolic phospholipase A2 (cPLA2), was initially isolated and characterized from bovine and human red blood cells
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| Product Name: | EA4 | | Synonyms: | EA4;7-chloro-6-[4-(diethylamino)phenyl]quinoline-5,8-dione;5,8-Quinolinedione, 7-chloro-6-[4-(diethylamino)phenyl]- | | CAS: | 389614-94-2 | | MF: | C19H17ClN2O2 | | MW: | 340.8 | | EINECS: | | | Product Categories: | | | Mol File: | 389614-94-2.mol |  |
| Boiling point | 508.3±50.0 °C(Predicted) | | density | 1.31±0.1 g/cm3(Predicted) | | storage temp. | -196°C | | solubility | ≤1mg/ml in DMSO;20mg/ml in dimethyl formamide | | form | crystalline solid | | pka | 6.14±0.44(Predicted) | | color | Light blue to blue |
| Uses | EA4, a derivative of quinone, is an inhibitor for both rPLA and cPLA. EA4 can inhibit rPLA2 with a Ki value of 130 μM. EA4 can be used for the research of hemostasis, thrombosis, and erythropoiesis[1]. | | Biological Activity | ki: 130 μmea4 is a rpla2 inhibitor.rpla2, a calcium-dependent cytosolic phospholipase a2 (cpla2), was initially isolated and characterized from bovine and human red blood cells. with a molecular mass of 42 kda, cpla2 shows biochemical properties similar to cpla2 type iv. | | in vitro | it was found that ea4 was able to inhibit a ca(2+) ionophore-induced arachidonic acid release from both human and bovine red blood cells, demonstrating that this enzyme was responsible for the ca(2+)-dependent arachidonic acid release from mammalian red blood cells [1]. another study found that in mouse hepatoma hepa-1c1c7 cells, ea4 could cause a significant induction of the cyp1a1-mediated ethoxyresorufin o-deethylase activity time- and concentration-dependently, and such induction was accompanied by an increase of the cyp1a1 mrna transcription. morevoer, in human cells including mcf-7 (human breast adenocarcinoma cell line), hepg2 (human hepatocarcinoma), and hl-60 (human promyelocytic cell line), the expression of cyp1a1 mrna could be also induced by ea4 treatment. in addition, cyp1b1 mrna was increased by ea4 in mcf-7 cells [2]. | | references | 1. shin, h.s.,chin, m.r.,kim, j.s., et al. purification and characterization of a cytosolic, 42-kda and ca2+-dependent phospholipase a2 from bovine red blood cells. the journal of biological chemisty 277, 21086-21094 (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. molecules and cells 12, 190-196 (2001). |
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