D609 (Synonyms: Tricyclodecan9yl xanthogenate) |
| Catalog No.GC17851 |
A competitive inhibitor of PC-specific PLC
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 83373-60-8
Sample solution is provided at 25 µL, 10mM.
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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:
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. >
| Cell experiment [1]: | |
|
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 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C 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. |
|
References: [1]. Paris L, Cecchetti S, Spadaro F, Abalsamo L, Lugini L, Pisanu ME, Iorio E, Natali PG, Ramoni C, Podo F. Inhibition of phosphatidylcholine-specific phospholipase C downregulates HER2 overexpression on plasma membrane of breast cancer cells. Breast Cancer Res. 2010;12(3):R27. | |
| Cas No. | 83373-60-8 | SDF | |
| Synonyms | Tricyclodecan9yl xanthogenate | ||
| Chemical Name | potassium O-(octahydro-1H-4,7-methanoinden-5-yl) carbonodithioate | ||
| Canonical SMILES | S=C(S[K])OC1CC2C3C(CCC3)C1C2 | ||
| Formula | C11H15KOS2 | M.Wt | 266.47 |
| Solubility | ≥ 35.33 mg/mL in DMSO with gentle warming, ≥ 24.5 mg/mL in EtOH with ultrasonic and warming, ≥ 12.7 mg/mL in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7528 mL | 18.7638 mL | 37.5277 mL |
| 5 mM | 0.7506 mL | 3.7528 mL | 7.5055 mL |
| 10 mM | 0.3753 mL | 1.8764 mL | 3.7528 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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