| EA4rPLA2 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity ≥ 95.00%
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- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 389614-94-2 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 7-chloro-6-[4-(diethylamino)phenyl]-5,8-quinolinedione | ||
| Canonical SMILES | CCN(CC)c1ccc(cc1)C1=C(Cl)C(=O)c2ncccc2C1=O | ||
| Formula | C19H17ClN2O2 | M.Wt | 340.8 |
| Solubility | ≤1mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Ki: 130 μM
EA4 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].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
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).
