Phospholipase A
Phospholipase A2 (PLA2) catalyzes sn-2 phospholipid hydrolysis, releasing fatty acids and lysophospholipids that support lipid metabolism and cell signaling[1]. Mechanistically, PLA2 activation supplies arachidonic acid for cyclooxygenase, lipoxygenase, and cytochrome P450 pathways, linking membrane phospholipid turnover to eicosanoid-driven inflammation[2]. In disease models, cPLA2α promotes lipid mediator production in human and rodent cells, and cPLA2α-deficient mice show reduced macrophage prostaglandin and leukotriene production, impaired fertility, and smaller postischemic brain injury[3][4]. Compared with related isoforms, cPLA2α is a widely expressed intracellular enzyme, whereas secreted PLA2, calcium-independent PLA2, and lipoprotein-associated PLA2 differ in localization, calcium requirement, and substrate context[1][2][5]. For experimental applications, pyrrophenone strongly inhibits cPLA2α activity, and AACOCF3 acts as a tight, slow-binding inhibitor of the 85-kDa human cytosolic PLA2[6][7].
References:
- [1]. Dennis EA, et al. Phospholipase A2 enzymes: physical structure, biological function, disease implication, chemical inhibition, and therapeutic intervention. Chem Rev. 2011 Oct 12;111(10):6130-85. [Content Brief]
- [2]. Mouchlis VD, et al. Phospholipase A2 catalysis and lipid mediator lipidomics. Biochim Biophys Acta Mol Cell Biol Lipids. 2019 Jun;1864(6):766-771. [Content Brief]
- [3]. Leslie CC. Cytosolic phospholipase A₂: physiological function and role in disease. J Lipid Res. 2015 Aug;56(8):1386-402. doi: 10.1194/jlr.R057588. Epub 2015 Apr 2. PMID: 25838312; PMCID: PMC4513982. et al. Cytosolic phospholipase A₂: physiological function and role in disease. J Lipid Res. 2015 Aug;56(8):1386-402. [Content Brief]
- [4]. Bonventre JV, et al. Reduced fertility and postischaemic brain injury in mice deficient in cytosolic phospholipase A2. Nature. 1997 Dec 11;390(6660):622-5. [Content Brief]
- [5]. Murakami M, et al. Updating Phospholipase A2 Biology. Biomolecules. 2020 Oct 19;10(10):1457. [Content Brief]
- [6]. Ono T, et al. Characterization of a novel inhibitor of cytosolic phospholipase A2alpha, pyrrophenone. Biochem J. 2002 May 1;363(Pt 3):727-35. [Content Brief]
- [7]. Street IP, et al. Slow- and tight-binding inhibitors of the 85-kDa human phospholipase A2. Biochemistry. 1993 Jun 15;32(23):5935-40. [Content Brief]
-
Phospholipase A Related Products (56)
Related Products (56)
-
Ochnaflavone
0 ImagesOchnaflavone is an inhibitor of IIA-type secretory phospholipase A2 (sPLA2-IIA) with an IC50 of 3.45 µM. Ochnaflavone exhibits significant anti-inflammatory and liver-protective effects, capable of inhibiting the degradation of phosphatidylethanolamine (PE) and lipid peroxidation induced by carbon tetrachloride (CCl4) in rat liver, with an IC50 of 7.16 µM for lipid peroxidation. Ochnaflavone can be used in research on liver damage and inflammatory diseases.
-
YM-26734
0 ImagesYM-26734 is a competitive inhibitor of secretory phospholipase A2 (PLA2) that exhibits a broad inhibitory profile to several PLA2s.
-
FKGK11
0 ImagesCat. No.: HY-116018CAS No.: 1071000-98-0FKGK11 is a potent and selective inhibitor of GVIA iPLA2 (Group VIA calcium-independent phospholipase A2). FKGK11 can be used for the research of ovarian cancer and neurological disorders such as peripheral nerve injury and multiple sclerosis.
-
LY433771
0 ImagesSynonyms: LSN433771LY433771 (LSN433771) (Compound 8) is a type X secretory phospholipase A2 (sPLA2) inhibitor with an IC50 value of 3 nM, which can be used in the study of cardiovascular diseases.
-
(Z)-Oleyloxyethyl phosphorylcholine
0 Images(Z)-Oleyloxyethyl phosphorylcholine ((Z)-OPC) is an isomer of Oleyloxyethyl phosphorylcholine (OPC). Oleyloxyethyl phosphorylcholine is an inhibitor of secreted Phospholipase A2 (sPLA2), which is involved in the biosynthesis of proinflammatory lipid media. Oleyloxyethyl phosphorylcholine can be used to study inflammatory diseases. Oleyloxyethyl phosphorylcholine also modified the red blood membrane and was used to bind the oxygen-carrying liquid perfluorocarbons as an antivenom agent to reduce toxin-induced hemolysis.
-
Efipladib
0 ImagesCat. No.: HY-106253CAS No.: 381683-94-9Efipladib is a potent, selective and orally active cPLA2α inhibitor with an IC50 of 0.04 μM and a Kd of 0.067 μM.
-
CAY10590
0 ImagesSynonyms: GK115CAY10590 (GK115) is an inhibitor of secreted phospholipase A2 (sPLA2) and can be used for the research of chronic inflammatory kidney diseases.
-
(2E)-OBAA
0 ImagesCat. No.: HY-101015CAS No.: 221632-26-4(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM.
-
Lp-PLA2-IN-2
0 ImagesCat. No.: HY-133148CAS No.: 2071636-15-0Lp-PLA2-IN-2 is a potent and selective lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2.
-
VI-60
0 ImagesCat. No.: HY-162228CAS No.: 3050874-42-2VI-60 is a dual, orally active inhibitor of cPLA2 and COX-2, which reveals an anti-inflammtory efficacy through the inhibition of p38 MAPK/cPLA2/COX-2/PGE2 pathway.
-
LY256548
0 ImagesCat. No.: HY-114873CAS No.: 107889-31-6Synonyms: LY25684LY256548 (LY25648) is an orally available anti-ischemic and anti-inflammatory compound with central nervous system activity. LY256548 is an inhibitor of phospholipase A2, 5-lipoxygenase (5-LOX), and COX, and inhibits A23187 (HY-N6687)-stimulated leukotriene B4 production. LY256548 inhibits bone damage and paw swelling in the rat Freund's complete adjuvant-induced arthritis (FCA) model.
-
PTAD-ergosta-3-one
0 ImagesCat. No.: HY-187095PTAD-ergosta-3-one is a snake venom enzyme inhibitor. PTAD-ergosta-3-one inhibits the procoagulant activity of citrated plasma mediated by serine protease (SVSP) from Bothrops asper venom. PTAD-ergosta-3-one inhibits the esterase activity of PLA2 from Bothrops asper venom. PTAD-ergosta-3-one can be used in the research of snakebite envenoming.
-
SB-435495 hydrochloride
0 ImagesCat. No.: HY-19415ACAS No.: 304694-41-5SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.
-
Protizinic acid
0 ImagesCat. No.: HY-106555CAS No.: 13799-03-6Protizinic acid is an orally active non-steroidal antiinflammatory agent with antiinflammatory and antipyretic activity. Protizinic acid inhibits phospholipase A2 (PLA2) activity, and the IC50 value is 210 μM.
-
PC(O-16:0/18:2(9Z,12Z))
0 ImagesCat. No.: HY-113507CAS No.: 88542-95-4PC(O-16:0/18:2(9Z,12Z)) is a phospholipid. PC(O-16:0/18:2(9Z,12Z)) serves as a substrate for Phospholipase A2.
-
Parameritannin A-1
0 ImagesCat. No.: HY-N16481CAS No.: 347406-26-2Parameritannin A-1 is a tetrameric proanthocyanidin (PAC) that can be isolated from the bark of Parameria laevigata Moldenke (Apocynaceae). Parameritannin A-1 is a COX-2 inhibitor. Parameritannin A-1 also inhibits the activity of phospholipase A2 (PLA2).
-
BAY-163
0 ImagesCat. No.: HY-184012CAS No.: 3134928-97-2BAY-163 is a tertiary urea derivative and inactive negative control probe for BAY-439 (HY-178123). BAY-163 does not inhibit phospholipase A2 group V (PLA2-G5) activity in immune cells. BAY-163 can be used for research on endometriosis.
-
AX048
0 ImagesCat. No.: HY-112738CAS No.: 873079-69-7AX048 is an inhibitor for calcium-dependent phospholipase A2 cPLA2 with a XI(50) of 0.022 mole fraction and reveals an antihyperalgesic efficacy.
-
BMS-229724
0 ImagesCat. No.: HY-120621CAS No.: 221914-85-8BMS-229724 is an orally active and tight-binding cytosolic phospholipase A2 (cPLA2) inhibitor with an IC50 of 2.8 μM. BMS-229724 can inhibit the production of arachidonic acid and eicosanoids in U937 cells, neutrophils, platelets, and other cells. BMS-229724 has anti-inflammatory activity and can be used in the research of diseases such as skin inflammation.
-
WAY-196025
0 ImagesCat. No.: HY-119094CAS No.: 540523-42-0WAY-196025 is a selective and orally active indole cytosolic phospholipase A2 alpha (cPLA2α) inhibitor with an IC50 of 0.01μM and a Kd of 0.013 μM. WAY-196025 can inhibit the production of prostaglandins (such as PGE2) and leukotrienes (such as LTB4), and reduce the release of inflammatory mediators. WAY-196025 can be used for the researches of inflammation and immunology, such as asthma.
