| Bioactivity | Pyrrophenone is a potent and specific cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 4.2 nM[1]. |
| Invitro | Pyrrophenone shows potent inhibition of arachidonic acid release, prostaglandin E2, thromboxane B2, and leukotriene B4 formation in human whole blood[1]. Pyrrophenone inhibits the production of arachidonic acid (AA) (IC50=24±1.7 nM), PGE2 (IC50=25±19 nM),, and LTC4 (IC50=14±6.7 nM),from THP-1 cells stimulated with A23187[1].Pyrrophenone inhibits the production of AA (IC50=0.19±0.068 μM), PGE2 (IC50=0.20±0.047 μM), TXB2 (IC50=0.16±0.093 μM),and LTB4 (IC50=0.32±0.24 μM) from human whole blood stimulated with A23187[1].Pyrrophenone (0.1-0.5 μM, 48 h) inhibits the growth of PC-PTC3 and PCCl3 cells[2]. Cell Proliferation Assay[2] Cell Line: |
| In Vivo | Pyrrophenone (administered i.p. at 20 mg/kg 30 min before LPS injection.) suppresses bronchoalveolar lavage (BAL) levels of leukotriene B4 (LTB4) and platelet activating factor (PAF)[3]. Animal Model: |
| Name | Pyrrophenone |
| CAS | 341973-06-6 |
| Formula | C49H37F2N3O5S2 |
| Molar Mass | 849.96 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| Reference | [1]. K Seno, et al. Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'. Bioorg Med Chem Lett. 2001 Feb 26;11(4):587-90. [2]. Stefania Mariggiò, et al. Cytosolic phospholipase A2 alpha regulates cell growth in RET/PTC-transformed thyroid cells. Cancer Res. 2007 Dec 15;67(24):11769-78. [3]. C-H Lee, et al. Mechanism of glutamine inhibition of cytosolic phospholipase a2 (cPLA2 ): Evidence of physical interaction between glutamine-Induced mitogen-activated protein kinase phosphatase-1 and cPLA2. Clin Exp Immunol. 2015 Jun;180(3):571-80. |
Pyrrophenone
CAS: 341973-06-6 F: C49H37F2N3O5S2 W: 849.96
Pyrrophenone is a potent and specific cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 4.2 nM.
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