VU0285655-1

SKU: orb1701478

Description

VU0285655-1 (BML-280) is a potent, selective phospholipase D2 (PLD2) inhibitor used in diabetic retinopathy research. It has been shown in vitro to inhibit high glucose-induced caspase-3 activation and loss of cell viability, supporting its application in studying metabolic disease-related cellular pathways.

Research Area

Cell Biology, Immunology & Inflammation, Metabolism Research

Key Properties

• CAS Number: 1158347-73-9
• MW: 429.51
• Purity: 99.73% (May vary between batches)
• Formula: C₂₅H₂₇N₅O₂
• SMILES: O=C1C2(N(CN1)C3=CC=CC=C3)CCN(CCNC(=O)C4=CC5=C(N=C4)C=CC=C5)CC2
• Target: Phospholipase,Interleukin,TNF
• Solubility: DMSO:50 mg/mL (116.41 mM)

Bioactivity

• 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. BML-280 inhibits mRNA levels and secretion of tumor necrosis factor-α, IL-1β and IL-8 in human periodontal ligament cells. VU0285655-1 shows an approximately 21-fold selectivity for PLD2. 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. 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.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BML280, BML-280, BML 280, Interleukin Related, PLD2, TNF, VU-0285655, VU0285655-1, VU 0285655

Compound Identifiers

PubChem CID

44138050