VU0359595  (Synonyms: CID-53361951; ML-270)

VU0359595 (CID-53361951; 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^[1][2][3][4].

VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells^[2].
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

497.43

C₂₅H₂₉BrN₄O₂

1246303-14-9

Solid

White to off-white

O=C([C@H]1[C@H](C2=CC=CC=C2)C1)N[C@@H](C)CN3CCC(N4C5=CC=C(Br)C=C5NC4=O)CC3

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]