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VU0285655-1

Catalog No. T26326   CAS 1158347-73-9
Synonyms: VU-0285655, VU0285655, BML 280, VU 0285655, BML280, BML-280

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.

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VU0285655-1 Chemical Structure
VU0285655-1, CAS 1158347-73-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 258.00
5 mg In stock $ 642.00
10 mg In stock $ 913.00
25 mg In stock $ 1,370.00
50 mg In stock $ 1,850.00
100 mg In stock $ 2,500.00
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Purity: 99.73%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
In vitro VU0285655-1 (BML-280) (0-5 µM; 24 h; Wild-type, PLD1- and PLD2-deficient astrocytes) reduces proliferation in PLD1-deficient cells, but also in PLD2-deficient cells exposed to IGF-1. BML-280 had minor effects in wild-type and PLD2-deficient cells but completely blocked PLD activity in PLD1-deficient cells. Caused a highly significant inhibition of glial proliferation when astrocytes were stimulated by FCS (fetal calf serum) or IGF-1, respectively. Showed non-specific effects because they inhibited cell proliferation even in PLD1/2 double knockouts at 5 µM.[1]
BML-280 inhibits mRNA levels and secretion of tumor necrosis factor-α, IL-1β and IL-8 in human periodontal ligament cells.[2]
VU0285655-1 shows an approximately 21-fold selectivity for PLD2.[3]
BML-280 (0-0.1 µM) suppresses formyl-Met-Leu-Phe (fMLP)-stimulated PLD activity in a concentration-dependent manner, with an IC50 of 0.04 ± 0.01 μM.[3]
BML-280 (0-0.3 µM) inhibits O2- generation, and the inhibition reaches a plateau (about 20 % inhibition) at around 0.01 μM to 0.3 μM.[3]
Synonyms VU-0285655, VU0285655, BML 280, VU 0285655, BML280, BML-280
Molecular Weight 429.51
Formula C25H27N5O2
CAS No. 1158347-73-9

Storage

store at low temperature

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

Solubility Information

DMSO: 50 mg/mL (116.41 mM)

TargetMolReferences and Literature

1. Burkhardt U, et al. Role of phospholipases D1 and 2 in astroglial proliferation: effects of specific inhibitors and genetic deletion. Eur J Pharmacol. 2015 Aug 15;761:398-404. 2. 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 Jul;184:243-257. 3. Tsai YR, et al. Inhibition of formyl peptide-stimulated phospholipase D activation by Fal-002-2 via blockade of the Arf6, RhoA and protein kinase C signaling pathways in rat neutrophils. Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):507-19.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Immunology/Inflammation Compound Library

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Keywords

VU0285655-1 1158347-73-9 Apoptosis Immunology/Inflammation Metabolism TNF Phospholipase Interleukin VU-0285655 VU0285655 BML 280 VU 0285655 BML280 BML-280 inhibitor inhibit

 

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