Phospholipase Inhibitor

Lp-PLA2-IN-12 (compound 19) is an Lp-PLA2 inhibitor. Lp-PLA2-IN-12 can be used for the study of neurodegenerative related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular disease including atherosclerosis.

cPLA2α-IN-2 (Compound 122) is an inhibitor of cytosolic phospholipase A₂α (cPLA₂α).

Folipastatin is a potent inhibitor of phospholipase A2 with an IC₅₀ of 39 μM. Folipastatin is a new depsidone compound from Aspergillus unguis.

Manoalogue is an irreversible secretory phospholipase A2 (sPLA2) inhibitor. Manoalogue covalently modifies K94 of bee venom phospholipase A2 (bvPLA2) to inactivate the enzyme and shows selective inhibition on bvPLA2. Manoalogue can suppress PLA2-mediated contractions of guinea pig lung pleural strips. Manoalogue is used for sPLA2 mechanism and respiratory physiology research.

Magnesium sulfate heptahydrate, meets analytical specification of Ph. Eur. BP USP FCC (Magnesium sulfate heptahydrate, meets analytical specification of Ph. Eur. BP USP FCC) is a hydrate of Magnesium sulfate (HY-Y1267) suitable for cell culture. Magnesium sulfate is a calcium antagonist and a potent L-type calcium channel inhibitor, as well as a uterine contraction inhibitor. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in research on diseases such as preeclampsia/eclampsia.

SMS2-IN-3 is a potent and selective SMS2inhibitor (IC₅₀=2.2 nM), significantly reduces the hepatic SM (22:0) levels.

SM (d18:1/15:0) is a sphingomyelinase inhibitor. SM (d18:1/15:0) is promising for research of neurodegenerative diseases (e.g., Alzheimer's) and metabolic syndrome.

MJ33-OH 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.

Lp-PLA2-IN-14 (Compound 19) is an Lp-PLA2 inhibitor with a pIC₅₀ of 8.4 against rhLp-PLA2. Lp-PLA2-IN-14 can be used for the research of neurodegenerative related diseases, such as Alzheimer Disease (AD), glaucoma, age-related macular degeneration (AMD) or cardiovascular diseases including atherosclerosis and the like.

U 84569 is a potent low-Km cAMP-dependent Phosphodiesterase inhibitor, with an IC₅₀ value of 300 nM in platelet cytosol. By inhibiting phosphodiesterase and elevating cAMP levels, U 84569 indirectly blocks receptor-mediated Phospholipase C activation, thereby inhibiting platelet aggregation.

Brinazarone (SR 33287) is an inhibitor for acid lysosomal sphingomyelinase, and leads to cellular lipidosis. Brinazarone potentiates the cytotoxic effects of anti-Thy 1.2 AT15E RTA-IT on T2 cells and anti-CD5 T101 on CEM cells.

sPLA2 inhibitor 2 (compound 6a) is a sPLA2 inhibitor, with IC₅₀ of 0.0475 μM. sPLA2 inhibitor 2 can be used in diabetes research.

SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA₂ inhibitor with an IC₅₀ of 0.06 nM.

PLC-β-IN-1 (Compound 8a) is a PLCβ inhibitor. PLC-β-IN-1 exerts anti-airway contraction activity by inhibiting PLCβ and its downstream signaling pathways, and can enhance the airway relaxation effect of β-agonists. PLC-β-IN-1 can be used in the study of asthma.

GNE-7056 is an orally active interleukin-2-inducible T-cell kinase (ITK) inhibitor with a K_i of 0.2 nM against human kinase, and exhibits high selectivity over LCK kinase. GNE-7056 inhibits PLCγ-1 phosphorylation, suppresses the production of IL-2, IL-4, IL-13 and TH2 cytokines, reduces CD4⁺ T-cell proliferation, and inhibits activation-induced cell death of CD4⁺ T cells by decreasing the abundance of FasL. GNE-7056 can be used in asthma-related research.

KARI 201 is a selective, brain penetrant pand competitive acid sphingomyelinase (ASM) inhibitor with an IC₅₀ of 338.3?nM. KARI 201 is a ghrelin receptor agonist. KARI 201 improves neuropathological features of Alzheimer's disease.

Me-Indoxam is a potent and cell-impermeable secreted phospholipase A₂ (sPLA₂) inhibitor.

DS07551382 is a potent phosphatidylserine synthase 1 (PTDSS1) inhibitor, thereby blocking intracellular phosphatidylserine synthesis. DS07551382 has antitumor activity.

A4333 is biotinylated compound of A3373 (HY-155342) that inhibits Phospholipase D1 (PLD1), but not PLD2. A4333 plays an important role in antitumor activity.

Avicin G is a sphingomyelinase inhibitor and plasma membrane disruptor. Avicin G inhibits the enzymatic activities of neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1), elevates intracellular sphingomyelin levels, and alters the distribution of sphingomyelin. Avicin G interferes with the lateral segregation of GTP- and GDP-bound H-Ras, inhibits the signal output of oncogenic K-Ras and H-Ras, reduces the phosphorylation of ERK and Akt, increases lysosomal pH, and inhibits the endocytic recycling of epidermal growth factor receptor. Avicin G can be used in research related to pancreatic ductal adenocarcinoma and non-small cell lung cancer.