Home Metabolism Phospholipase (e.g. PLA)

Phospholipase (e.g. PLA)

Secreted phospholipases A2 (sPLA2) belongs to phospholipases A2 (PLA2) which is a group of enzymes that cleave fatty acids from the glycerol. sPLA2 can be expressed in different kinds of cells including mouse spermatogenic cells, spermatozoa,interstitial Leydig cells, and epithelium of the epididymis, vasdeferens, seminal vesicles, and prostate. sPLA2, which needs to be activated by Ca2+, has a role in amplifying the action of cPLA2αwhich was activated by p38 MAP kinase and ERK in the early phase and by ERK alone in the late phase in supplying arachidonic acid for eicosanoid production.

Other Metabolism Related Inhibitors

Dehydrogenase Transferase DPP Aminopeptidase Procollagen C Proteinase P450 (e.g. CYP17) Factor Xa PDE DHFR Carbonic Anhydrase

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S1110 Varespladib (LY315920) Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM, and it has reached Phase 3.
Journal of the American Heart Association, November 13, 2015, e002553
PLoS One, April 20, 2015, e0119088
Int J Mol Sci, 2024, 25(19)10649
Verified customer review of Varespladib (LY315920)
S7520 Darapladib (SB-480848) Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.
Antimicrob Agents Chemother, 2025, e0047125.
iScience, 2024, 27(12):111404
iScience, 2024, 27(5):109774
S7609 GW4869 GW4869 (GW69A, GW554869A) is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM, also is a commonly used exosome inhibitor.
J Extracell Vesicles, 2025, 14(2):e70042
Proc Natl Acad Sci U S A, 2025, 122(8):e2421717122
NPJ Biofilms Microbiomes, 2025, 11(1):113
Verified customer review of GW4869
S8011 U-73122 U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO).
EMBO Rep, 2025, 10.1038/s44319-025-00444-2
Front Immunol, 2025, 16:1491928
Cancer Cell Int, 2025, 25(1):408
Verified customer review of U-73122
S2364 Tanshinone I Tanshinone I, an active principle isolated from Salvia miltiorrhiza (Danshen), is structurally similar to tanshinone IIA and may possess similar cytotoxic effects on tumor cells.
Int J Oncol, 2023, 63(1)76
Phytomedicine, 2022, 98:153958
Drug Des Devel Ther, 2022, 16:3197-3213
Verified customer review of Tanshinone I
S4255 Quinacrine 2HCl Quinacrine 2HCl(Quinacrine dihydrochloride) is a lipophilic cationic drug with multiple actions that is commonly used as an anti-protozoal agent. Quinacrine is an effective phospholipase A2 inhibitor.
Viruses, December 30, 2022, 105
Molecules, August 29, 2022, 5561
Viruses, 2022, 105
S2390 (E/Z)-Polydatin (E/Z)-Polydatin is a mixture of cis- and trans-configurations of Polydatin.
Phytotherapy Research, 2025, Online ahead of print
Heliyon, 2024, 10(21):e39933
International Journal of Oncology, 2024, 77
S9794 Melittin Melittin (MLT, Forapin, Forapine) is an activator of phospholipase A2 (PLA2) that stimulates the activity of the low molecular weight PLA2, while it does not the increase the activity of the high molecular weight enzyme.
Molecular Medicine Reports, October 18, 2024, 5
Cell Death and Disease, August 8, 2024, 573
Cell Death & Disease, August 08, 2024, 573
S3220 Trigonelline Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. This compound inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. It also inhibits the microtubule formation in RBL-2H3 cells.
Respiratory Research, June 15, 2024, 242
International Journal of Medical Sciences, February 18, 2025, 1194-1207
Biochemistry and Biophysics Reports, April 21, 2025, 102021
S7321 FIPI FIPI (5-Fluoro-2-indolyl deschlorohalopemide), a derivative of halopemide, is a potent and selective inhibitor of phospholipase D with IC50 of 25 nM and 20 nM for PLD1 and PLD2, respectively.
Cancer Cell Int, 2025, 25(1):408
Cell Chem Biol, 2024, S2451-9456(24)00090-4
Nature Communications, 2021, 5042

Signaling Pathway Map