Phospholipase 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.

Pyrrophenone (Standard) is the analytical standard of Pyrrophenone (HY-111376). This product is intended for research and analytical applications. Pyrrophenone is a potent and specific cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC₅₀ value of 4.2 nM.

Darapladib analog-1 (Compound 16) is an O-alkylated Darapladib (HY-10521). Darapladib analog-1 inhibits Lp-PLA₂. Darapladib analog-1 can be used in the research of atherosclerosis.

DO53 is a serine hydrolase inhibitor that targets ABHD6, PAFAH2, PLA2G7, ABHD2 and CES1C. DO53 reduces LPS (HY-D1056A1)-induced cytokine production in the mouse brain, decreases fasting-induced refeeding behavior, and induces hypoactivity in mice. As a DAGL negative control, DO53 shows no activity against DAGLα/β in vivo, and does not affect brain lipid levels, DSE/DSI synaptic plasticity or LPS-induced anhidrosis in mice. DO53 can be used in studies related to LPS-induced neuroinflammation and fasting-induced refeeding.

BAPTA tetrapotassium (Standard) is the analytical standard of BAPTA tetrapotassium (HY-100168B). This product is intended for research and analytical applications. BAPTA tetrapotassium is a selective and cell-impermeant chelator for calcium. BAPTA tetrapotassium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca²⁺ release from intracellular stores or influx via Ca²⁺-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca²⁺ chelators.

SMases D-IN-1 is an inhibitor of SMase D (sphingomyelinase D) from Loxosceles (brown recluse spider), with a K_i value of 0.54 μM. SMases D-IN-1 inhibits the hydrolysis of sphingomyelin substrates by recombinant and native SMases D, reduces the binding ability of SMases D to human red blood cells, and prevents the shedding of glycophorin C from the surface of human red blood cells. SMases D-IN-1 partially inhibits Loxosceles venom-induced death of human keratinocytes and also suppresses systemic reactions triggered by Loxosceles venom. SMases D-IN-1 can be used in studies related to recluse spider envenomation.

CCT129957 (Standard) is the analytical standard of CCT129957 (HY-111208). This product is intended for research and analytical applications. CCT129957 is an indole derivative and a potent phospholipase C-γ (PLC-γ) inhibitor with an IC₅₀ of ~3 μM and a GC50 of 15 μM. CCT129957 inhibits Ca2+ release in squamous carcinoma cells at ~15 μM.