D609

Short Summary : PC-PLC inhibitor

Category : Apoptosis|PC-PLC

Purity : 0.98

CAS Number : 83373-60-8

Formula : C11H15KOS2

Molecular Weight : 266.47

SMILE : S=C(S[K])OC1CC2C3C(CCC3)C1C2

Solubility : >12.7mg/mL in DMSO

Storage : Store at -20°C

Description : D609 is a specific and competitive inhibitor of phosphatidylcholine-specific phospholipase C (PC-PLC) with a Ki value of 6.4 M. [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 g/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 g/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 g/mL) and IL-1 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:1. a) E. Amtmann, Drugs Exp Clin Res 1996, 22, 287-294; b) R. M. Adibhatla, J. F. Hatcher and A. Gusain, Neurochem Res 2012, 37, 671-679. 2. L. Paris, S. Cecchetti, F. Spadaro, L. Abalsamo, L. Lugini, M. E. Pisanu, E. Iorio, P. G. Natali, C. Ramoni and F. Podo, Breast Cancer Res 2010, 12, R27. 3. a) K. Tschaikowsky, M. Meisner, F. Schonhuber and E. Rugheimer, Br J Pharmacol 1994, 113, 664-668; b) R. R. Cobb, K. A. Felts, G. C. Parry and N. Mackman, Mol Pharmacol 1996, 49, 998-1004. >

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