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]
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Phospholipase A Related Products (56)
Related Products (56)
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Cacospongionolide B
0 ImagesCat. No.: HY-N21818CAS No.: 172854-76-1Cacospongionolide B is an orally active sesterterpene compound that can be isolated from Fasciospongia cavernosa. Cacospongionolide B is a secreted phospholipase A2 (sPLA2) inhibitor with an IC50 of 4.3 μM. Cacospongionolide B exhibits antibacterial activity. Cacospongionolide B downregulates the expression of iNOS, COX-2 and TNF-α by inhibiting NF-κB nuclear translocation and its DNA binding, and simultaneously selectively and irreversibly inhibits sPLA2 enzymatic activity. Cacospongionolide B can be used in studies related to bacterial infection and adjuvant arthritis.
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ML256
0 ImagesCat. No.: HY-128762CAS No.: 2415152-07-5ML256 is a covalent lipoprotein-associated phospholipase A2 (Lp-PLA2 inhibitor. ML256 can be used for the study of neoplasms harboring a constitutively active variant of one or both of KRAS or HRAS.
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AGN-190383
0 ImagesCat. No.: HY-165327CAS No.: 120755-15-9AGN-190383 is a bee venom phospholipase A2 inhibitor. AGN 190383 inhibits both hormone-operated and depolarization-dependent calcium mobilization as well as fMLP stimulated increases in free cytosolic calcium. AGN-190383 has anti-inflammatory activity.
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Ro 23-9358
0 ImagesCat. No.: HY-108132CAS No.: 153125-17-8Ro 23-9358 is a potent secretory phospholipase A2 inhibitor with anti-inflammatory activity.
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Manoalogue
0 ImagesCat. No.: HY-182680CAS No.: 136440-42-1Manoalogue is an irreversible secretory phospholipase A2 (sPLA2) inhibitor. Manoalogue covalently modifies K94 of bee venom phospholipase A2 (bvPLA2) to inactivate the enzyme and shows selective inhibition on bvPLA2. Manoalogue can suppress PLA2-mediated contractions of guinea pig lung pleural strips. Manoalogue is used for sPLA2 mechanism and respiratory physiology research.
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Lp-PLA2-IN-14
0 ImagesCat. No.: HY-153560CAS No.: 2756855-66-8Lp-PLA2-IN-14 (Compound 19) is an Lp-PLA2 inhibitor with a pIC50 of 8.4 against rhLp-PLA2. Lp-PLA2-IN-14 can be used for the research of neurodegenerative related diseases, such as Alzheimer Disease (AD), glaucoma, age-related macular degeneration (AMD) or cardiovascular diseases including atherosclerosis and the like.
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SB-435495 ditartrate
0 ImagesCat. No.: HY-19415BCAS No.: 304694-43-7SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.
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LY 178002
0 ImagesLY 178002 is a potent inhibitor of 5-lipoxygenase (5-LPO), phospholipase A2, with IC50 of 0.6 μM for 5-lipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.
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Me-Indoxam
0 ImagesCat. No.: HY-125157CAS No.: 172732-62-6Me-Indoxam is a potent and cell-impermeable secreted phospholipase A2 (sPLA2) inhibitor.
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(R)-Bromoenol lactone-d7
0 ImagesCat. No.: HY-117068SSynonyms: (R,E)-Bromoenol lactone-d7(R)-Bromoenol lactone-d7 ((R,E)-Bromoenol lactone-d7) is the deuterated-labeled (R)-Bromoenol lactone (HY-117068). (R)-Bromoenol lactone ((R,E)-Bromoenol lactone) is an isomer of Bromoenol lactone (HY-107411). (R)-Bromoenol lactone acts as a selective inhibitor of microsomal calcium-independent phospholipase A2γ (iPLA2γ). (R)-Bromoenol lactone induces mild activation of p38 mitogen-activated protein kinase in prostate cancer cells, resulting in slight increases in the expressions of phosphorylated p53, total p53 and p21. (R)-Bromoenol lactone is applicable to prostate cancer-related research.
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PLA2-IN-1
0 ImagesCat. No.: HY-173335PLA2-IN-1 (Compound 7) is a potent and selective inhibitor of phospholipase A2 (PLA2) with an IC50 value of 1 nM PLA2-IN-1 inhibits PLA2-induced coagulopathy in vitro. PLA2-IN-1 is promising for research of snakebite envenomation caused by cobra venom.
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Cinatrin C2
0 ImagesCat. No.: HY-N14104CAS No.: 136266-36-9Cinatrin C2 is a phospholipase A2 (PLA2) inhibitor with an IC50 of 800 μM and can be extracted from Circinotrichum falcatisporum RF-641.
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CGP-33304 sodium
0 ImagesCat. No.: HY-117385CAS No.: 111130-14-4CGP-33304 sodium is an antagonist of the leukotriene receptor and an inhibitor of phospholipase A2. CGP-33304 sodium inhibits the accumulation of myocardial depressant factor (MDF) activity in plasma and prolongs survival time in a standardized traumatic shock model of rats. CGP-33304 sodium can be applied in the research of traumatic shock.
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Cinatrin C3
0 ImagesCat. No.: HY-N14105CAS No.: 136266-37-0Cinatrin C3 is a phospholipase A2 (PLA2) inhibitor with an IC50 of 70 μM and can be extracted from Circinotrichum falcatisporum RF-641.
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Darapladib analog-1
0 ImagesCat. No.: HY-120849CAS No.: 1389264-17-8Darapladib analog-1 (Compound 16) is an O-alkylated Darapladib (HY-10521). Darapladib analog-1 inhibits Lp-PLA2. Darapladib analog-1 can be used in the research of atherosclerosis.
