| Bioactivity | D609, an antitumoural xanthate, is a specific and competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor with a Ki of 6.4 μM. D609 is an antioxidative protector and has antiviral and anti-inflammatory activity[1][2][3]. | ||||||||||||
| Target | Ki: 6.4 μM (PC-PLC) | ||||||||||||
| Invitro | D609 (100 μM; for 2 h) significantly attenuats the proliferation of various cell lines[2]. D609 (50, 100 and 200 μM; for 2 h) results in caspase-3 activation with 200 μM and causes no detectable cleavage with 50, 100 μM[2]. D609 (100 μM; for 2 h) significantly inhibits BrdU incorporation in BV-2 microglia and causes accumulation of cells in G1 phase with decreased number of cells in the S phase[2]. D609 (100 μM; for 2 h and cultured for an additional 2 h or 22 h without D609) increases ceramide levels, up-regulates p21 expression and causes a decreases in phospho-Rb[2]. Cell Proliferation Assay[2] Cell Line: | ||||||||||||
| In Vivo | D609 (2.5, 10 mg/kg/day; ip; for 6 weeks) inhibits the progression of preexisting atherosclerotic lesions in apoE-/- mice and changes the lesion composition into a more stable phenotype[3]. D609 (50 mg/kg; ip; single dose) for 30 min before intratracheal administration of LPS (3 mg/kg) prevents the development of LPS-induced pulmonary hypertension in adult male Wistar rats[4]. Animal Model: | ||||||||||||
| Name | D609 | ||||||||||||
| CAS | 83373-60-8 | ||||||||||||
| Formula | C11H15KOS2 | ||||||||||||
| Molar Mass | 266.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. E Amtmann, et al. The antiviral, antitumoural xanthate D609 is a competitive inhibitor of phosphatidylcholine-specific phospholipase C. Drugs Exp Clin Res. 1996;22(6):287-94. [2]. Gusain A, et al. Anti-proliferative effects of tricyclodecan-9-yl-xanthogenate (D609) involve ceramide and cell cycle inhibition.Mol Neurobiol. 2012 Jun;45(3):455-64. Epub 2012 Mar 14. [3]. Lu Zhang, et al. D609 inhibits progression of preexisting atheroma and promotes lesion stability in apolipoprotein e-/- mice: a role of phosphatidylcholine-specific phospholipase in atherosclerosis. Arterioscler Thromb Vasc Biol. 2010 Mar;30(3):411-8. [4]. Rachele Pandolfi, et al. Role of acid sphingomyelinase and IL-6 as mediators of endotoxin-induced pulmonary vascular dysfunction. Thorax. 2017 May;72(5):460-471. [5]. Kalluri HS, et al. D609 inhibits the proliferation of neural progenitor cells.Neuroreport. 2010 Jul 14;21(10):700-3. |