Phospholipase Inhibitor

1-Naphthaleneacetic acid (Standard) is the analytical standard of 1-Naphthaleneacetic acid. This product is intended for research and analytical applications. 1-Naphthaleneacetic acid (1-Naphthylacetic acid), a auxin, can promote plant growth. 1-Naphthaleneacetic acid is also an inhibitor of PLA2, with an IC50 of 13.16 μM.

SMase-IN-1 (Compound 4) is a bacterial sphingomyelinase enzyme (SMase) inhibitor (IC₅₀ value for B. cereus SMase is 6.43 µM). SMase-IN-1 also inhibits eqBuChE (59.50% inhibition rate at 50 µM concentration). SMase-IN-1 forms a complex with Cu²⁺ in biometal interactions. SMase-IN-1 reduces B. cereus-induced hemolysis on sheep erythrocytes.

m-3M3FBS (Standard) is the analytical standard of m-3M3FBS. This product is intended for research and analytical applications. m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis.

CGP-33304 sodium is an antagonist of the leukotriene receptor and an inhibitor of phospholipase A₂. CGP-33304 sodium inhibits the accumulation of myocardial depressant factor (MDF) activity in plasma and prolongs survival time in a standardized traumatic shock model of rats. CGP-33304 sodium can be applied in the research of traumatic shock.

Cinatrin C3 is a phospholipase A2 (PLA2) inhibitor with an IC₅₀ of 70 μM and can be extracted from Circinotrichum falcatisporum RF-641.

VU0155056 is a cell-permeable phospholipase D inhibitor.

CGP-43182 is a secretory phospholipase A2 group II (sPLA2) inhibitor with an IC₅₀ of 2.8 μM. CGP-43182 binds to the active site of the enzyme, blocks IL1β-stimulated gene expression and NFκB activation, and inhibits the production of prostaglandin and nitric oxide (NO). CGP-43182 exhibits anti-inflammatory activity in multiple inflammatory models and can be used for studies on adjuvant arthritis, carrageenan-induced edema, pertussis pleurisy, and glomerular inflammatory responses.

Varespladib (Standard) is the analytical standard of Varespladib. This product is intended for research and analytical applications. Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.

GW4869 (Standard) is the analytical standard of GW4869 (HY-19363). This product is intended for research and analytical applications. GW4869 is a noncompetitive neutral sphingomyelinase (N-SMase) inhibitor with an IC₅₀ of 1 μM. GW4869 is an inhibitor of exosome biogenesis/release.

HpFabZ-IN-1 (Compound 1) is an inhibitor of the key enzyme FabZ in the Helicobacter pylori fatty acid synthesis pathway, with its IC₅₀ value being 39.8 µM. HpFabZ-IN-1 does not possess antibacterial activity.

Malabaricone C is an orally active and noncompetitive sphingomyelin synthase (SMS) inhibitor with IC50 values of 3 μM and 1.5 μM for SMS 1 and SMS 2, respectively. Malabaricone C reduces body weight gain, improves glucose tolerance, and decreases lipid accumulation in the liver, showing significant prevention of high fat diet-induced fatty liver in mice. Malabaricone C has anti-inflammatory effects, which is found in the fruits of Myristica cinnamomea King. Malabaricone C is promising for research of obesity and immunological disorders caused due to hyper-activation of T-cells.

ARF1 (2-17) inhibits both ARF-independent (PLC-β) and ARF-dependent (PLD) pathways. ARF1 (2-17) inhibits GTP-γ-S-stimulated PLD activity, phospholipase C-β (PLC-β), and exocytosis.

Difluprednate (Standard) is the analytical standard of Difluprednate. This product is intended for research and analytical applications. Difluprednate is a topical corticosteroid, which is thought to act by the induction of phospholipase A2 inhibitory proteins (lipocortins). Difluprednate is used for the symptomatic treatment of inflammation and pain associated with ocular surgery.

Darapladib (Standard) is the analytical standard of Darapladib. This product is intended for research and analytical applications. Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer.

Halopemide (Standard) is the analytical standard of Halopemide. This product is intended for research and analytical applications. Halopemide is a potent phospholipase D (PLD) inhibitor, with IC50s of 220 and 310 nM for human PLD1 and PLD2, respectively. Halopemid is a dopamine receptors antagonist, and acts a psychotropic agent.

Cinatrin B has the activity of inhibiting phospholipase A2.

Ro 31-4639 is a potent phospholipase A2 inhibitor with an IC₅₀ of 1.5 μM.

AK106-001616 is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2) (IC₅₀=3.8 nmol/L). AK106-001616 is able to reduce the production of prostaglandins (PG) E2 and leukotrienes (LT) B4 by stimulated cells. AK106-001616 can be used in the study of inflammatory diseases, neuropathic pain and pulmonary fibrosis.

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

U-73122 (Standard) is the analytical standard of U-73122 (HY-13419). This product is intended for research and analytical applications. U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC₅₀of 1-2.1 µM for PLC.