pld1

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).

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.

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.

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.

A4333, a biotinylated derivative of A3373, selectively inhibits Phospholipase D1 (PLD1) while sparing PLD2. It is noted for its significant role in antitumor activity [1].

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.

Desketoraloxifene is a selective estrogen receptor modulator, inhibiting mammalian PLD (PLD1 and PLD2).

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].

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).

VU0155056 is a dual PLD1 2 inhibitor with IC50 = 81 nM for PLD1 and IC50 = 240 nM for PLD2 in in vitro assays, and IC50 < 1 µM in cellular assays, which inhibits breast cancer cell invasion.

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].