| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
Cell lines | HER2-overexpressing SKBr3 cells and various cancer cells |
Preparation method | The solubility of this compound in DMSO is >12.7 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months. |
Reacting condition | 50 μg/mL |
Applications | D609 inhibited PC-PLC, which enhanced HER2 internalization and lysosomal degradation, inducing down-regulation of HER2 expression on the membrane. Moreover, D609-induced PC-PLC inhibition significantly delayed HER2 re-expression on the membrane and reduced the overall cellular contents of HER2, HER2-HER3 and HER2-EGFR heterodimers. In addition, D609 also exhibited antiproliferative effects, especially in Trastuzumab-resistant cells, via PC-PLC inhibition. In breast cancer cells, D609 at the dose of 50 μg/mL decreased the activity of PC-PLC by 3.5 folds within 1hr. |
| 产品描述 | D609 is a specific and competitive inhibitor of phosphatidylcholine-specific phospholipase C (PC-PLC) with a Ki value of 6.4 μM. [1] PC-PLC hydrolyzes (phosphatidylcholine) PC to generate 1, 2-diacylglycerol (DAG) and phosphocholine. D609 is a widely known inhibitor of PC-PLC and also inhibit sphingomyelin synthase (SMS). Due to these actions, it has antiviral and antitumor properties. D609 does not inhibit bacterial phosphatidylinositol (PI)-PLC, bovine pancreatic PLA2 or phospholipase D from cabbage[1b]. In OVCAR3 cells treated with (53 μg/mL) for 24 h, PC-PLC activity was significantly inhibited and cell proliferation was affected. In breast cancer cells, the activity of PC-PLC decreased 3.5 fold after the incubation with D609 (50 μg/ml) within 1h. The human epidermal growth factor receptor 2 (HER2) was also down-regulated [2]. D609 also has anti-inflammatory functions. It blocked the nitric oxide synthase induced by LPS (IC50=20 μg/mL) and IL-1β induced vascular cell adhesion molecule 1 gene expression in human endothelial cells.[3] D609 can reduce sphingomyelin synthase, thereby it inhibits bFGF-stimulated astrocyte proliferation. Because of the presence of the thiol function, D609 also has antioxidant/glutathione mimetic properties[1b]. References: |
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