Phospholipase Inhibitor

LCL521 dihydrochloride is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).

YM-26734 is a competitive inhibitor of secretory phospholipase A² (PLA²) that exhibits a broad inhibitory profile to several PLA2s.

ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A₂ (sPLA₂s) with an IC₅₀ of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca²⁺-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for researching inflammation related diseases.

N-Stearoylsphingomyelin (N-Stearoyl-D-sphingomyelin) is a sphingolipid, which can inhibit Phospholipase Cδ1 (PLCδ1).

FKGK11 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.

SPK-601 (LMV-601) is an inhibitor of the phosphatidylcholine-specific phospholipase C (PC-PLC). SPK-601 also can be used as an antimicrobial agent.

ARC39 is an acid sphingomyelinase (ASM) inhibitor.

Fuzapladib (IS-741) sodium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib sodium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib sodium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site.

Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC₅₀ of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2).

LY433771 (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 ((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 is a potent, selective and orally active cPLA₂α inhibitor with an IC₅₀ of 0.04 μM and a K_d of 0.067 μM.

MJ33-OH lithium is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.

CAY10590 (GK115) is an inhibitor of secreted phospholipase A₂ (sPLA₂) and can be used for the research of chronic inflammatory kidney diseases.

EA4, a derivative of quinone, is an inhibitor for both rPLA and cPLA. EA4 can inhibit rPLA₂ with a K_i value of 130 μM. EA4 can be used for the research of hemostasis, thrombosis, and erythropoiesis.

AZD2716 is an orally active secretory phospholipase A₂ (sPLA₂) inhibitor. AZD2716 inhibits human GIIA sPLA₂ (IC₅₀=10 nM), human GV sPLA₂ (IC₅₀=40 nM), human GX sPLA₂ (IC₅₀=400 nM), snake venom sPLA₂ (IC₅₀=2 pM), and snake (Bothrops jararacussu) Lys49-PLA2-like toxin (K_d=110 μM). AZD2716 inhibits sPLA₂ isoforms IIa, V, X, snake venom sPLA₂s, and snake venom Lys49-PLA₂-like toxin myotoxic activity via hydrophobic channel binding. AZD2716 suppresses GIIA sPLA₂ production, neutralizes snake venom-induced myotoxicity, and improves survival in envenomed mice. AZD2716 can be used for the research of coronary artery disease, atherosclerosis, and snakebite envenoming.

RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC₅₀ is 54 μM) and VHR (IC₅₀ is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC₅₀s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24.

Luffariellolide is an inhibitor of human synovial fluid phospholipase A2 (HSF-PLA2) (IC₅₀=5 μM). Luffariellolide effectively inhibits phorbol ester (PMA)-induced ear edema (ED₅₀=50 μg/ear).

(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.

Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC₅₀s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.