- 貨號 Cat. No.
- T-750
- 規格 Size
- 0.2 mg 5x0.2mg 1mg
Description
Triacsin C
Acyl CoA Synthase Inhibitor
Sizes: |
0.2 mg |
5 x 0.2 mg |
1 mg |
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Bioassay: |
Triacsin C inhibits the proliferation of 3T3L1 cells. |
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3T3L1 cells were treated with different concentrations of Triacin C (#T-750) for 3 days; the number of live cells was measured by XTT cell proliferation assay kit, normalized to the control (100 %) and plotted against drug concentration.
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1.
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Yoshida, K. et al. (1982) J. Antibiot. (Tokyo) 35, 151. |
2.
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Omura, S. et al. (1986) J. Antibiot. (Tokyo) 39, 1211. |
3.
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Tomoda, H. et al. (1987) Biochim. Biophys. Acta. 17, 595. |
4.
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Tomoda, H. et al. (1991) J. Biol. Chem. 266, 4214. |
5.
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Hartman, E.J. et al. (1989) Prostaglandins 37, 655. |
Triacsin C is a fungal metabolite from Streptomyces aureofaciens1 which almost completely inhibits de novo synthesis of triacylglycerol and phospholipid.2,3 This compound specifically inhibits the activity of long chain acyl-CoA synthetase 1 and 4 (IC50~8mM) but has no effect on the activity of acyl-CoA synthetase 5, in intact cells and in cell lysates. Inhibition of these enzymes causes a decrease in the cellular levels of acyl-CoA precursors for lipid synthesis activity, cell proliferation and lipid transformation.4 Kinetic analysis indicates that inhibition of acyl-CoA synthetase by Triacsin C is not competitive with respect to the two substrates of acyl-CoA synthetase (ATP and coenzyme A), but is competitive with respect to long-chain fatty acids. The N-hydroxytriazene moiety of Triacsin C has been suggested to be essential for the inhibitory activity against acyl-CoA synthetase.2-4
Triacsin C arrests the metabolism of arachidonic acid by inhibition of arachidonoyl-CoA synthetase thus interfering in the production of prostaglandins and in the regulation of blood pressure.5
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