SB 204990

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Description: ATP citrate lyase (ACLY) inhibitor
Chemical Name: (3R,5S)-rel-5-[6-(2,4-Dichlorophenyl)hexyl]tetrahydro-3-hydroxy-2-oxo-3-furanacetic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Reviews

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries for SB 204990

SB 204990 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SB 204990

M. Wt 389.27
Formula C18H22Cl2O5
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 154566-12-8
PubChem ID 10340264
InChI Key YTRNLFYTHYWDAU-KDOFPFPSSA-N
Smiles ClC(C=C(Cl)C=C2)=C2CCCCCC[C@@H](OC1=O)C[C@]1(O)CC(O)=O

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
Solubility
DMSO 38.93 100
ethanol 38.93 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for SB 204990

Certificate of Analysis / Product Datasheet
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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


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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:

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

Greenwood et al (2022) Acly Deficiency Enhances Myelopoiesis through Acetyl Coenzyme A and Metabolic–Epigenetic Cross-Talk Immunohorizons 6 837 PMID: 36547387


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