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VU0359595

Catalog No. T21777 CAS 1246303-14-9

Synonyms: VU0359595-1, CID-53361951, ML-270

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

VU0359595, CAS 1246303-14-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 98.00
5 mg	In stock	$ 232.00
10 mg	In stock	$ 339.00
25 mg	In stock	$ 572.00
50 mg	In stock	$ 818.00
100 mg	In stock	$ 1,130.00

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Purity: 99.15%

Biological Description

Chemical Properties

Storage & Solubility Information

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, at concentrations ranging from 5 to 5000 nM, inhibits both the baseline and FCS/IGF-1 stimulated proliferation of astroglial cells. At doses of 5, 50, and 500 nM, with a 30-min exposure, it does not impact the basal phospholipase D (PLD) activity in astrocytes; however, it significantly reduces mitogen-stimulated PLD activity in a concentration-dependent manner[2]. Additionally, at a concentration of 0.15 μM administered 1 h before and during a 4 h high glucose treatment, VU0359595 notably decreases the high glucose-induced increase in [3H]-phosphatidylethanol (PEth) generation in retinal pigment epithelium (RPE) cells[3]. When applied at 5 μM one hour before lipopolysaccharide (LPS) treatment, it modulates autophagy in LPS-induced RPE cells undergoing a 24-h treatment with 10 μg/ml of LPS[4]. Furthermore, a 2 nM pre-exposure for 30 min effectively blocks the gliotoxin (50 ng/ml)-enhanced internalization of A. fumigatus in A549 cells[5].

Synonyms	VU0359595-1, CID-53361951, ML-270
Molecular Weight	497.43
Formula	C25H29BrN4O2
CAS No.	1246303-14-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (10.1 mM), Sonification is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Bioactive Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max

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Keywords

VU0359595 1246303-14-9 Metabolism Phospholipase VU0359595-1 CID-53361951 ML270 ML 270 VU-0359595 CID 53361951 CID53361951 VU 0359595 ML-270 inhibitor inhibit

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