Home Metabolism Phospholipase (e.g. PLA)

Phospholipase (e.g. PLA) Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
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
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
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
S6564 ML348 ML348 (GNF-Pf-1127) is a potent and selective APT1 (Acyl protein thioesterase 1)/lysophospholipase 1 (LYPLA1) inhibitor with Ki values of 280 nM and >10 μM for APT1 and APT2, respectively.
Science Signaling, 2025, eadr2008
Nature Biomedical Engineering, 2019, 306-317
S6522 ST 271 ST271 is a tyrphostin-like protein tyrosine kinase (PTK) inhibitor which inhibits phospholipase D (PLD) activity.
S9478 Trans-4-Phenyl-3-buten-2-one Trans-4-Phenyl-3-buten-2-one (trans-Benzylideneacetone, trans-Benzalacetone, trans-Benzylideneacetone) is an inhibitor of the enzyme phospholipase A2 (PLA2). This compound is used as a flavouring agent, a fragrance and a bacterial metabolite.
E1116 AACOCF3 AACOCF3 (Arachidonyl trifluoromethyl ketone) is an inhibitor of cytosolic phospholipase A2 (cPLA2) and calcium-independent phospholipase A2(iPLA2) with IC50 of 1.5 μM and 6.0 μM, respectively. It inhibits aortic osteoinductive signalling and vascular calcification in the cholecalciferol-overload mouse model.
E1765 U-73343 U-73343 is an inactive analog of U-73122 that acts downstream of phospholipase C and inhibits receptor-mediated phospholipase D (PLD) activation in CHO-CCK_A cells.
S5913 Cambinol Cambinol is a novel uncompetitive nSMase2 inhibitor with a K i value of 7 μM (IC50 = 5 ± 1 μM).
E8148 BAPTA BAPTA is a Ca²⁺ chelator and an inhibitor of phospholipase C (PLC) with an IC50 of 7.0 mM and exhibits high Ca²⁺ selectivity, minimal pH dependence, and a fast binding rate. Its rapid Ca²⁺ buffering capacity makes it ideal for studying Ca²⁺ release from intracellular stores or influx through Ca²⁺ channels.
E8206 CAY10650 CAY10650 is a potent inhibitor of cytosolic phospholipase A2α (cPLA2α), with an IC50 of 12 nM. It exhibits anti-inflammatory effects in a murine contact dermatitis model.
S0766 RHC 80267 RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. This compound inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC).