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Phospholipase Inhibitors

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SML0904 ABO dihydrochloride ≥98% (HPLC) ABO is a modulator of Annexin A7 (ANXA7) GTPase, a member of the annexin family of calcium/phospholipid-binding proteins. ABO can directly bind to Annexin A7 and inhibit its phosphorylation. Annexin A7 is involved in several processes especially in the process of membrane fusion and exocytosis. ABO is a GTPase, and both GTP-binding and Protein kinase C (PKC) activity are important in regulating its function to potentiate calcium-dependent membrane fusion. Annexin A7 has several other activities, not fully understood. ABO suppressed oxidized low-density lipoprotein (oxLDL)-induced phosphatidylcholine-specific phospholipase C (PC-PLC) activity, inhibiting apoptosis and promoting autophagy in vascular endothelial cells, indicating that ANXA7 is an endogenous regulator of phosphatidylcholine-specific phospholipase C (PC-PLC). ABO significantly reduced atherosclerotic plaque area and reduced lipid deposition and pro-inflammatory macrophages in apolipoprotein E-/- mice. ABO should be a valuable tool to study the complex functions of Annexin 7.
896126-03-7 (free base)
SML1913 ASB14780 ≥98% (HPLC) New ASB14780 is an indole-based selective and potent cytosolic phospholipase A2α inhibitor (IC50 = 20 nM/cPLA2α and >10 μM/sPLA2α). ASB14780 inhibits cPLA2α-dependent inflammatory responses both in cultures and in animals in vivo, including LPS-induced PGE2 production (IC50 = 0.5 μM; mouse peritoneal exudate cells), A23187-induced TXB2 production (IC50 = 0.54 and 0.64 μM using guinea pig and human whole blood, respectively), TPA-induced ear edema (50 mg/kg, p.o.; mice), OVA-induced asthma (5 - 20 mg/kg/d, p.o.; guinea pig), CCl4-induced hepatic fibrosis and high-fat cholesterol diet-induced fatty liver (0.1-0.3 g/kg/d, p.o.; mouse). SB14780 bioavailability is also demonstrated in dog and monkey, albeit at a lower value (F = 34.3%/dog and 30.9%/monkey vs. 89.6%/mouse).
1069046-00-9
SML0856 AT-56 ≥98% (HPLC) AT-56 is a selective orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), one of two synthases involved in the production of Prostaglandin D2 (PGD2) from arachidonic acid. PGD2 is a lipid signaling molecule, which activates two receptors, DP1 involved in centrally mediated processes such as sleep and pain, and DP2 involved and inflammation. The two PGD synthases involved in its synthesis are hematopoietic (H-PDGS) and lipocalin-type (L-PGDS), which acts to form PGD2 in the CNS and other systems but not in inflammatory cells/tissues. AT-56 binds competitively at the enzyme′s catalytic pocket, and has no effect on the production of other PGs or H-PDGS-catalyzed PDG2. AT-56 inhibited PGD2 production by L-PGDS-expressing human TE-671 cells with an IC50 value of 3 μM without affecting production of PGE2 and PGF2, but had no effect on the PGD2 production by H-PGDS-expressing human megakaryocytes.
162640-98-4
A9451 Aristolochic acid I sodium salt powder, ≥97% Component of some Chinese herbal medicines, and responsible for their nephrotoxicity. Prodrug activated by reduction of the nitro group to an amine, which forms cytotoxic DNA adducts.
10190-99-5
A5512 Aristolochic acid I powder Potent phospholipase A2 inhibitor, including calcium ionophore-induced phospholipase A2 activity in neutrophils. Kidney tumor initiator in experimental animal model.
313-67-7
B1552 Bromoenol lactone ≥98% (TLC) Potent, irreversible inhibitor of calcium-independent phospholipase A2 and of magnesium-dependent phosphatidate phosphohydrolase from P388D macrophages (IC50 = 8 μM); enzyme activated irreversible chymotrypsin inhibitor (Ki = 636 nM).
88070-98-8
C5241 Cinnamycin from Streptomyces cinnamoneus, ≥95% (HPLC) Cinnamycin is a tetracyclic polypeptide antibiotic containing 19 amino acids. The polypeptide has the unusual amino acids threo-3-methyl-lanthionine, meso-lanthionine, lysinoalanine and 3-hydroxyaspartic acid. It is produced by Streptomyces cinnamoneus and belongs to the duramycin-type l antibiotics. Lantibiotics are synthesized in the ribosome and undergo extensive post-translational modifications to attain their active antimicrobial form. The unique receptor for Cinnamycin, phosphatidylethanolamine (PE), is located on the inner leaflet of the plasma membrane. Cinnamycin induces transbilayer lipid movement leading to the exposure of PE to the outer leaflet of the plasma membrane. The interaction of Cinnamycin with PE provides a tool for PE monitoring. Cinnamycin is active against Gram-positive rods such as Bacilli, Clostyridium and Mycobacterium, causing cell wall biosynthesis stress.
Cinnamycin, like other lantibiotics, was also reported to inhibit phospholipase A2 (PLA2). It was suggested as an alternative treatment for atherosclerosis through its ability to inhibit PLA2 by binding to its substrate PE. Moreover, Cinnamycin was found to inhibit Herpes simplex virus (HSV-1) activity.
110655-58-8
C2313 Compound 48/80 Promotes release of histamine. Inhibits calmodulin and activates G proteins.
 
C0256 Cytidine 5′-diphosphocholine sodium salt dihydrate ~98%, from yeast, solid Neuroprotective in situations of hypoxia and ischemia; biosynthetic intermediate of membrane phospholipids; cerebral vasodilator; inhibits PLA2 activation.
33818-15-4
F5807 FIPI hydrochloride hydrate ≥98% (HPLC), powder FIPI is a potent Phospholipase D (PLD) inhibitor. The signaling enzyme Phospholipase D (PLD) and the lipid second messenger phosphatidic acid (PA) generated by PLD are implicated in many cell biological processes including Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI is a potent in vivo inhibitor of both PLD1 and PLD2, setting the stage for a new era of exploration and validation of cell biological roles for mammalian PLD. It rapidly blocks in vivo PA production with sub-nM potency. FIPI inhibits PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis, indicating potential utility for it as a therapeutic for autoimmunity and cancer metastasis. It does not affect PLD subcellular localization, PIP2 availability, the actin stress fiber network in resting CHO cells, or selected signaling events proximal to PLD activation.
FIPI is a potent phospholipase D (PLD) inhibitor effective at sub-nM levels. Phospholipase D (PLD) and the lipid second messenger phosphatidic acid (PA) generated by PLD are implicated in many cell biological processes including Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI inhibits both PLD1 and PLD2, rapidly blocking in vivo PA production. FIPI inhibits PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis, suggesting potential as a therapeutic for autoimmune diseases and cancer metastasis.
 
SML0707 FKGK11 ≥98% (GC) FKGK11 is a potent inhibitor of GVIA iPLA2 with little or no inhibition against GIVA cPLA2 (XI(50) = 0.0073 and >0.91, respectively). The compound displays a slight inhibition against GVsPLA2. FKGK11 potently inhibited the progression and severity in a murine experimental autoimmune encephalomyelitis (EAE) model.
1071000-98-0
SML0857 HQL 79 ≥98% (HPLC) HQL-79 is a selective inhibtor of hematopoietic prostaglandin D (PGD) synthase, one of two synthases involved in the production of Prostaglandin D2 (PGD2) from arachidonic acid. PGD2 is a lipid signaling molecule, which activates two receptors, DP1 involved in centrally mediated processes such as sleep and pain and DP2 involved and inflammation. The two PGD synthases involved in its synthesis are lipocalin-type (L-PGDS) and hematopoietic (H-PDGS), which acts to form PGD2 in mast cells, Th2 cells, microglia, and other inflammatory cells/tissues. HQL-79 selectively inhibited the activity of recombinant H-PGDS with an IC50 of 6 μM and had almost no effect on COX-1, COX-2, m-PGES, or L-PGDS up to 300 μM. HQL-79 has anti-inflammatory activity in vitro and in vivo.
162641-16-9
H3041 Halopemide ≥98% (HPLC) Halopemide is a dopamine receptor antagonist and a phospholipase D2 inhibitor. Halopemide may be used as a screen to identify inhibitors of human PLD2 using an in vitro biochemical assay. It is also inhibitory at benzodiazepine binding sites.
59831-65-1
L6795 LY311727 ≥98% (HPLC), powder LY311727 is an orally active; potent secretory Phospholipase A2 (sPLA2; Group IIa) inhibitor.
164083-84-5
M3315 MJ33 lithium salt powder, ≥90% (NMR) Novel, active site directed, specific, competitive and reversible inhibitor of phospholipase A2 (PLA2).
199106-13-3
SML1004 ML211 ML211 is a very potent, dual inhbitor of lysophospholipase 1 (LYPLA1; IC50 = 17 nM) and lysophospholipase 2 (LYPLA2; IC50 = 30 nM).
 
SML1077 ML298 ≥98% (HPLC) ML298 is a potent, specific inhibitor of Phospholipase D2 (PLD2; IC50 = 355 nM). ML298 does not affect PLD1 activity at concentrations up to 20 μM.
1426916-02-0
M2939 Methyl arachidonyl fluorophosphonate ≥98%, methyl acetate solution (10 mg/mL) MAFP is a selective, irreversible inhibitor of both calcium-dependent and calcium-independent cytosolic phospholipase A2, but not secretory phospholipase A2. MAFP is also a potent acetylcholinesterase inhibitor.
 
M2689 Methyl γ-linolenyl fluorophosphonate ≥98%, methyl acetate solution An analog of MAFP which has been widely studied as an inhibitor of phospholipases, FAAH, and as a cannabinoid receptor ligand.
 
A8486 N-(p-Amylcinnamoyl)anthranilic acid ≥98% (HPLC) Broad spectrum phospholipase A2 (PLA2) inhibitor and TRP channel blocker.
99196-74-4
T8543 O-Tricyclo[5.2.1.02,6]dec-9-yl dithiocarbonate potassium salt ≥95%, solid D609 can block the production of diacylglycerol (DAG) in the cell. D609 functions by inhibiting the phospholipase C-mediated hydrolysis of the phosphate bond present in phosphatidylcholine and other glycerophospholipids.
Phosphatidylcholine-specific phospholipase C (PLC) and HIV-1 inhibitor. Xanthogenate derivative with in vitro anti-tumor activity.
83373-60-8
O0766 ONO-RS-082 ≥97% (HPLC) ONO-RS-082 is a reversible phospholipase A2 inhibitor.
99754-06-0
U6756 U-73122 hydrate powder Inhibits the hydrolysis of PPI to IP3, which leads to a decrease in cytosolic free calcium. Inhibits the coupling of G protein-phospholipase C activation, while remaining unaffected by production of cAMP.
112648-68-7 (anhydrous)
U6881 U-73343 Inactive analog of U73122; used as a negative control.
142878-12-4
V8639 VO-OHpic trihydrate ≥98% (HPLC), solid VO-OHpic trihydrate is a PTEN (phosphatase and tensin homologue deleted on chromosome 10) inhibitor.
476310-60-8
SML0566 VU0359595 ≥97% (HPLC) VU0359595 is a PLD1 specific inhibitor with an IC50 of 3.7 nM, and 1500-fold selectivity over PLD2 (IC50 = 6.4 μM).
1246303-14-9
SML1100 Varespladib ≥98% (HPLC) Varespladib is a potent and selective inhibitor of secretory phospholipase A2 (sPLA2). The compound Varespladib inhibits both human and mouse sPLA2 group IIA, V, and X enzymes at low nM concentrations.
172732-68-2
SML1226 YM-26734 ≥95% (HPLC) YM-26734 is a competitive inhibitor of the secreted (Group II) form of phospholipase A2. The IC50 against rabbit platelet derived sPLA2 is 85 nM. YM-26734 is active against, but less potent for group I (pancreatic) sPLA2 (porcine pancreatic enzyme IC50 = 7 μM), and does not inhibit intracellular PLA2 isoforms.
144337-18-8