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]