BML-280 (VU0285655-1) 是一种有效的选择性磷脂酶 D2 (PLD2) 抑制剂。BML-280 能够防止高糖诱导的 caspase-3 裂解和细胞活力降低。BML-280 可用于类风湿关节炎的研究。
| 生物活性 | BML-280 (VU0285655-1) is a potent and selectivephospholipaseD2 (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[1][2]. |
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体外研究
(In Vitro) | BML-280 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 IC50of 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].
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)[1].
BML-280 inhibits mRNA levels and secretion of tumor necrosis factor-α, IL-1β and IL-8 in human periodontal ligament cells[2].
Cell Proliferation Assay[1] | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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