VU0285655-1

Research use only, not for human use.

VU0285655-1(BML-280) is a potent and selective phospholipase D2 (PLD2) inhibitor that inhibits the proliferation of PLD2-deficient cells.

BML-280 (VU0285655-1) is a potent and selective phospholipase D2 (PLD2) inhibitor. BML-280 has the ability to prevent caspase-3 cleavage and reduction in cell viability induced by high glucose. BML-280 can be used for rheumatoid arthritis research.

BML-280 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.BML-280 (0-5 μM, 24 h) reduces proliferation in PLD1-deficient cells, but also in PLD2-deficient cells exposed to IGF-1 (Insulin-like growth factor 1). BML-280 inhibits mRNA levels and secretion of tumor necrosis factor-α, IL-1β and IL-8 in human periodontal ligament cells.Cell Proliferation Assay Cell Line:Wild-type, PLD1- and PLD2-deficient astrocytes Concentration:0, 50, 500, and 5000 nM Incubation Time:24 h Result: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.

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Metabolic Enzyme/Protease

Phospholipase

Phospholipase | Interleukin | TNF

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1158347-73-9

429.51

C25H27N5O2

>98% (HPLC)

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O=C1C2(N(CN1)C3=CC=CC=C3)CCN(CCNC(=O)C4=CC5=C(N=C4)C=CC=C5)CC2

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(-20℃)

With Ice Pack

≥ 2 years