Potent (IC50 = 44 nM) and selective inhibitor of acetyl-CoA synthetase 2 (ACSS2), an enzyme that is upregulated in nutrient-stressed cancer cells.1 It completely blocked fatty acid synthesis from acetate in SKBR3 breast cancer cells. VY-3-135 caused growth inhibition of mouse and human triple negative breast cancer cells that expressed high levels of ACSS2 but not those that expressed low levels. It displayed no effects on gene regulation.
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