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VY-3-135 is an orally active, stable and specific acetyl-CoA synthetase 2 (ACSS2) inhibitor with IC50 of 44 nM, showing no inhibitory activity against recombinant human ACSS1 or ACSS3. VY-3-135 can effectively inhibit ACSS2-dependent fatty acid metabolism but has no effect on gene expression in tumors.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 92 € | In Stock | |
5 mg | 187 € | In Stock | |
10 mg | 311 € | In Stock | |
25 mg | 530 € | In Stock | |
50 mg | 748 € | In Stock | |
100 mg | 1.064 € | In Stock | |
500 mg | 2.118 € | In Stock | |
1 mL x 10 mM (in DMSO) | 227 € | In Stock |
Description | VY-3-135 is an orally active, stable and specific acetyl-CoA synthetase 2 (ACSS2) inhibitor with IC50 of 44 nM, showing no inhibitory activity against recombinant human ACSS1 or ACSS3. VY-3-135 can effectively inhibit ACSS2-dependent fatty acid metabolism but has no effect on gene expression in tumors. |
In vitro | METHODS: BT474 cells were treated with VY-3-135 (0.01, 0.1, 1 μM), and SKBr3 cells were treated with VY-3-135 (1 μM). RESULTS VY-3-135 completely blocked fatty acid synthesis from acetate in SKBr3 cells. VY-3-135 is an effective targeted ACSS2 inhibitor in cells. [1] |
In vivo | METHODS: BT474-transplanted mice were randomly assigned and treated with VY-3-135 (100 mg/kg) by intraperitoneal (IP) injection or oral gavage. Tumor size was measured in mice. RESULTS VY-3-135 inhibited the growth of MDA-MB-468 (ACSS2 high) tumors but had no effect on WHIM12 (ACSS2 low) tumors. [1] |
Molecular Weight | 429.51 |
Formula | C26H27N3O3 |
Cas No. | 1824637-41-3 |
Smiles | CCn1c(nc2ccc(cc12)C(=O)NC[C@@H](C)O)C(O)(c1ccccc1)c1ccccc1 |
Relative Density. | 1.21 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (116.41 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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