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ATP citrate lyase (ACLY) inhibitor. Prodrug of SB 201076. Inhibits cholesterol and fatty acid synthesis in a dose-dependent manner in HepG2 cells. Orally active in vivo.
Sold for research purposes under agreement from GlaxoSmithKline
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 389.27. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.57 mL||12.84 mL||25.69 mL|
|5 mM||0.51 mL||2.57 mL||5.14 mL|
|10 mM||0.26 mL||1.28 mL||2.57 mL|
|50 mM||0.05 mL||0.26 mL||0.51 mL|
References are publications that support the biological activity of the product.
Pearce et al (1998) The role of ATP citrate-lyase in the metabolic regulation of plasma lipids. Hypolipidaemic effects of SB-204990, a lactone prodrug of the potent ATP citrate-lyase inhibitor SB-201076. Biochem.J. 334 113 PMID: 9693110
Gribble et al (1998) ATP-Citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R*,5S*)-ω-substituted-3-carboxy-3, 5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzy J.Med.Chem. 41 3582 PMID: 9733484
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Keywords: SB 204990, SB 204990 supplier, SB204990, ATP-citrate, lyases, ACL, inhibitors, inhibits, prodrug, SB-201076, cholesterol, fatty, acid, metabolic, lipids, synthases, transferases, ACLY, ATP, Citrate, Lyase, 4962, Tocris Bioscience
3 Citations for SB 204990
Citations are publications that use Tocris products. Selected citations for SB 204990 include:
Shah et al (2016) Targeting ACLY sensitizes castration-resistant prostate cancer cells to AR antagonism by impinging on an ACLY-AMPK-AR feedback mechanism. Oncotarget 7 43713 PMID: 27248322
Chen et al (2018) Compartmentalized activities of the pyruvate dehydrogenase complex sustain lipogenesis in prostate cancer. Nat Genet 50 219 PMID: 29335542
Namgaladze et al (2018) Polarization of Human Macrophages by Interleukin-4 Does Not Require ATP-Citrate Lyase. Front Immunol 9 2858 PMID: 30568658
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Reviews for SB 204990
Average Rating: 5 (Based on 1 Review.)
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SB-204990 were used as an ACLY inhibitor in subconfluent endothelial cells. The images are shown in the publication PubMed ID 29429925.
Literature in this Area
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