Phospholipase Inhibitor

PLD-IN-1 (Compound 3r) is an orally active inhibitor for phospholipase D with an IC₅₀ of 1.97 μM. PLD-IN-1 reduces the expression of CD24, CD47 and PD-L1, enhances the calreticulin expression, and thus modulates the immune evasion mechanism in lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the cell viability of lung cancer cell A549, HCC44, H460 and HCC15 with IC₅₀ of 18.44, 22.31, 24.85 and 21.45 μM, respectively. PLD-IN-1 can induce apoptosis and inhibits migration in cell A549. PLD-IN-1 enhances the level of pro-inflammatory M1 macrophages and decreases the level of anti-inflammatory M2 macrophages, exhibits antitumor efficacy in mouse model.

GK187 is a potent and selective Group VIA calcium-independent phospholipase A₂ (GVIA iPLA₂) inhibitor with an X_I(50) value of 0.0001. GK187 can be used for researching various neurological disorders.
^{[The X_I(50) is the mole fraction of the inhibitor in the total substrate interface required to inhibit the enzyme by 50%.]}

Tanshinone I (Standard) is the analytical standard of Tanshinone I. This product is intended for research and analytical applications. Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC₅₀=11 μM) and rabbit recombinant cPLA2 (IC₅₀=82 μM).

Lansoprazole sodium (AG 1749 sodium) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole sodium (AG 1749 sodium) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

(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.

Neomycin, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin is a known phospholipase C (PLC) inhibitor. Neomycin potently inhibits both the nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis. Neomycin inhibits IP3-mediated Ca²⁺ release, MgATP-dependent Ca²⁺ uptake, and electrical excitation-evoked skeletal muscle Ca²⁺ transients. Neomycin depletes gut microbiota in specific mouse models, causes hearing impairment, and kidney damage with prolonged exposure. Neomycin can be used for the research of cancer.

sPLA2-X Inhibitor 31 is a selective secreted phospholipase A₂ type X (sPLA₂-X) inhibitor with IC₅₀s of 26 nM, 310 nM, and 2230 nM for sPLA₂-X, sPLA₂-IIa, and sPLA₂-V, respectively.

PF-04217903 phenolsulfonate is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a K_i value of 4.8 nM and a K_d value of 4.5 nM. PF-04217903 phenolsulfonate blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 phenolsulfonate suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 phenolsulfonate retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 phenolsulfonate increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 phenolsulfonate is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis).

FIPI hydrochloride is a phospholipase D (PLD) inhibitor with an IC₅₀ for PLD1 and PLD2 of about 25 nM. FIPI hydrochloride regulates cytoskeletal recombination, cell diffusion and chemotaxis. FIPI hydrochloride can be used in cancer research. In addition, FIPI hydrochloride can enhance the secretion and aggregation of platelet dense particles, inhibit thrombosis, reduce ischemic stroke infarct volume and improve nerve function.

Lp-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.

Aristolochic acid C (Standard) is the analytical standard of Aristolochic acid C. This product is intended for research and analytical applications. Aristolochic acid C is a derivative of Aristolochic acid. Aristolochic acid is a phospholipase A2 (PLA2) inhibitor, which disrupts cortical microtubule arrays and root growth in Arabidopsis.

trans-Benzylideneacetone (Standard) is the analytical standard of trans-Benzylideneacetone. This product is intended for research and analytical applications. trans-Benzylideneacetone (trans-Benzalacetone), a metabolite of gram-negative entomopathogenic bacterium Xenorhabdus nematophila, is an enzyme inhibitor against phospholipase A2 (PLA2). trans-Benzylideneacetone is an immunosuppressant[1].

Plipastatin A1 (Fengycin IX; SNA-60-367-3) is a lipopeptide with phospholipase A2 inhibitory activity. Plipastatin A1 inhibits conidial germination of Botrytis cinerea in vitro and reduces the incidence of gray mold on tomato leaves. Plipastatin A1 is applicable to research related to gray mold^[1][2].

RK-682 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A). RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium 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 hemicalcium 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[2].

ZPL-5212372 (PF 5212372) is a cPLA2α inhibitor (IC₅₀ = 7 nM). ZPL-5212372 inhibits the release of prostaglandin D2 (PGD2), cysteyl leukotrienes, leukotriene B4, thromboxane A2, and PGD2 from human lung cells. ZPL-5212372 inhibits delayed bronchoconstriction and airway hyperresponsiveness in a sheep allergic inflammation model. ZPL-5212372 may be used in asthma research.

MJ-33 is a competitive phospholipase A₂ (PLA₂) inhibitor with an IC₅₀ of 0.3 μM. MJ-33 inhibits the activation of NOX2 by blocking the PLA₂ activity of Prdx6, thereby reducing the production of ROS. MJ-33 effectively inhibits the activity of acidic PLA₂ (pH 4.0), reduces the degradation of pulmonary surfactant phosphatidylcholine (PC), but has no effect on alkaline PLA₂ (pH 8.5). MJ-33 significantly alleviates lung oxidative damage induced by ischemia-reperfusion (I/R). MJ-33 significantly inhibits the invasive, migratory and adhesive abilities of prostate cancer cells by suppressing the MAPK, AKT, NF-κB and AP-1 signaling pathways. MJ-33 can be used to study ROS-related diseases and prostate cancer.

VI-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 (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 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.

Lansoprazole (Standard) is the analytical standard of Lansoprazole. This product is intended for research and analytical applications. Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).