| Description | 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. |
| In vitro | VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells. VU0359595 (5, 50, 500 nM; 30 min) does not affect basal PLD activity in astrocytes but reduces mitogen-stimulated PLD activity in a concentration-dependent manner[2]. VU0359595 (0.15 μM; 1 h before high glucose treatment and 4 h during high glucose treatment) partially reduces the increase [3H]-phosphatidylethanol (PEth) generation induced by high glucose (33 mM) in retinal pigment epithelium (RPE) cells[3]. VU0359595 (5 μM; 1 h prior to LPS treatment) modulates the autophagic process of LPS-induced (10 μg/ml; 24 h) RPE cells[4]. VU0359595 (2 nM; pretreatment 30 min) blocks the increase of A. fumigatus internalization induced by 50 ng/ml gliotoxin in A549 cells[5]. |
| Synonyms | VU0359595-1, CID-53361951, ML-270 |
| molecular weight | 497.43 |
| Molecular formula | C25H29BrN4O2 |
| CAS | 1246303-14-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 4.98 mg/mL (10 mM), Sonication is recommended. |
| References | 1. Lewis JA, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009;19(7):1916-1920. 2. Burkhardt U, et al. Phospholipase D is a target for inhibition of astroglial proliferation by ethanol. Neuropharmacology. 2014;79:1-9. 3. Tenconi PE, et al. High glucose-induced phospholipase D activity in retinal pigment epithelium cells: New insights into the molecular mechanisms of diabetic retinopathy. Exp Eye Res. 2019;184:243-257. 4. Bermúdez V, et al. Lipopolysaccharide-Induced Autophagy Mediates Retinal Pigment Epithelium Cells Survival. Modulation by the Phospholipase D Pathway. Front Cell Neurosci. 2019;13:154. Published 2019 Apr 24. 5. Jia X, et al. Gliotoxin promotes Aspergillus fumigatus internalization into type II human pneumocyte A549 cells by inducing host phospholipase D activation. Microbes Infect. 2014 Jun;16(6):491-501. |