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Biological Activity for SB 204990
SB 204990 is an ATP citrate lyase (ACLY) inhibitor; it is a prodrug of SB 201076. SB 204990 inhibits cholesterol and fatty acid synthesis in a dose-dependent manner in HepG2 cells. Suppresses growth of cancer cells showing aerobic glycolysis in vitro and in vivo. Orally active.
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries for SB 204990
Technical Data for SB 204990
|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.
Solubility Data for SB 204990
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for SB 204990
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 for SB 204990
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
Hatzivassiliou et al (2005) ATP citrate lyase inhibition can suppress tumor cell growth. Cancer Cell 8 311 PMID: 16226706
If you know of a relevant reference for SB 204990, please let us know.
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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
6 Citations for SB 204990
Citations are publications that use Tocris products. Selected citations for SB 204990 include:
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
Greenwood et al (2022) Acly Deficiency Enhances Myelopoiesis through Acetyl Coenzyme A and Metabolic–Epigenetic Cross-Talk Immunohorizons 6 837 PMID: 36547387
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
Yuesheng et al (2022) The short-chain fatty acid acetate modulates epithelial-to-mesenchymal transition. Mol Biol Cell 33 PMID: 35544303
Guido et al (2020) Phosphorylation of eukaryotic initiation factor-2α (eIF2α) in autophagy. Cell Death Dis 11 433 PMID: 32513922
Do you know of a great paper that uses SB 204990 from Tocris? Please let us know.
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