pld

VU533 (Nape-Pld activator) is a NAPE-PLD activator with an EC50 value of 0.30 µM.VU533 enhances NAPE-PLD activity and increases macrophage cytosolic burial.VU533 may be used in diseases associated with cardiometabolism.

LEI-401 is a selective and potent NAPE-PLD inhibitor that crosses the blood-brain barrier (IC50: 27 nM).LEI-401 reduces the level of n-acylethanolamines (NAEs) in the brain of free-ranging mice and modulates their emotional behaviour.

VU534 is a NAPE-PLD agonist with an EC50 of 0.30 μM.VU534 is a dual inhibitor of FAAH and sEH, with an IC50 of 1.2 μM for sEH.VU534 is used in diseases related to cardiometabolism.

PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.

PLD1 inhibitor is a compound that targets phospholipase D1 (PLD1). It suppresses PLD activity in A549 cells overexpressing PLD1 with an IC50 of 1.97 µM. This inhibitor also decreases the viability of A549 lung cancer and HCT116 colorectal cancer cells, with IC50 values of 18 and 29 µM, respectively. Furthermore, it impairs proliferation, migration, and invasion of A549 cells and triggers apoptosis. Administered at 10 mg/kg every other day, PLD1 inhibitor diminishes tumor growth, induces intratumoral apoptosis, and lowers levels of Ras, CD47, CD24, and programmed cell death 1 ligand 1 (PD-L1) in a murine Lewis lung carcinoma model.

ARN19874 is a selective, reversible uncompetitive inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity, with an IC50 of approximately 34 μM[1].

Icofungipen is an oral antifungals with active against Candida species.

Halopemide is a potent inhibitor of PLD (IC50 = 220 and 310 nM for human PLD1 and PLD2). Halopemid is an antagonist of dopamine receptors. Halopemid can be used in psychotropic research.

VU0359595 (ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases.

ML299 (VU0463568) is a dual PLD1/2 inhibitor (PLD1 and PLD2, IC50 of 6 nM, 20 nM, respectively).

Neomycin sulfate (Framycin sulfate) is a broad-spectrum aminoglycoside antibiotic that blocks the synthesis of bacterial proteins in order to exert antimicrobial activity. Neomycin sulfate is commonly used to screen prokaryotic and eukaryotic cells for Neo resistance genes.

VU0285655-1(BML-280) is a potent and selective phospholipase D2 (PLD2) inhibitor that inhibits the proliferation of PLD2-deficient cells.VU0285655-1 has an inhibitory effect on high glucose-induced caspase-3 cleavage and reduction of cell viability.VU0285655-1 is used in the study of diabetic retinopathy.

FIPI (5-Fluoro-2-indolyl deschlorohalopemide) is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM); prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.

VU0155069 hydrochloride (CAY10593 hydrochloride) is a potent and selective inhibitor of phospholipase D (PLD), exhibiting IC50 values of 46 nM for PLD1 and 933 nM for PLD2. It effectively inhibits the migration of both human and mouse breast cancer cell lines [1] [2].

Sonidegib diphosphate (LDE225 diphosphate) is a selective antagonist of Smo that inhibits murine Smo (IC50:1.3 nM) and human Smo (IC50:2.5 nM).

VU0155069 strongly inhibits the invasive migration of several cancer cell lines in transwell assays. VU0155069 is a selective phospholipase D1 inhibitor (IC50: 46 nM in vitro).

Sonidegib (Erismodegib), a Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.

VU 0364739 hydrochloride (VU 0364739 HCl) is a selective and potent inhibitor of phospholipase D2 (PLD2) with IC50s of 20 and 1500 nM for PLD2 and PLD1, respectively.VU 0364739 hydrochloride exhibits potential anticancer activity and induces apoptosis. VU 0364739 hydrochloride has potential anticancer activity, induces apoptosis, and can be used in the study of cancer and metabolic-related diseases.

CAY10594 is a potent phospholipase D2(PLD2) inhibitor. CAY10594 ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis.

A3373 is a novel inhibitor targeting both Phospholipase D1 (PLD1) and Phospholipase D2 (PLD2), demonstrating half maximal inhibitory concentrations (IC50) of 325 nM for PLD1 and 15.15μM for PLD2. This compound effectively suppresses lipopolysaccharide (LPS)-induced immune responses and is implicated in key processes of autoimmune arthritis, bone demineralization, and osteoclastogenesis [1] [2].

ML-298 (CID53393915) is a potent, specific inhibitor of Phospholipase D2 (PLD2, IC50 of 355 nM).

L-Cysteinesulfinic acid is an endogenous neurotransmitter with agonistic effects on a variety of metabotropic glutamate receptors (mGluRs), including mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, with a pEC50 = 2.7 to 4.0. L- Cysteinesulfinic acid is a pld-coupled agonist of metabotropic excitatory amino acid (EAA) receptors.

Dioctanoylphosphatidic acid sodium (DOPA sodium) is a bioactive phosphatidic acid (PA) derivative serving as a key lipid signaling molecule. Derived from glycerophospholipids via the action of phospholipase D (PLD), it acts as a precursor to diacylglycerol (DAG) and lysophosphatidic acid (LPA). It specifically binds to and activates the FRB domain of the mammalian target of rapamycin (mTOR), thereby promoting mTOR phosphorylation. Additionally, it modulates the respiratory burst in phagocytic cells such as neutrophils. In oncological studies, it has been shown to enhance the viability of gallbladder cancer (GBC) cells inhibited by histone deacetylase inhibitors (HDACI), suggesting a protective role against epigenetic-mediated growth suppression.

CHS-111 is a benzyl indazole compound that inhibits superoxide anion (O(2)(-)) generation and reduces fMLP-stimulated PLD activity (IC(50) 3.9±1.2μM). It inhibits the interaction of PLD1 with ADP-ribosylation factor (Arf) 6 and Ras homology (Rho) A, and reduces the membrane recruitment of RhoA in fMLP-stimulated cells.