Definition

An orally bioavailable small molecule inhibitor of the enzyme human acetyl coenzyme A synthetase short chain family member 2 (ACSS2; acetyl CoA synthetase 2), with potential antineoplastic activity. Upon oral administration, the ACSS2 inhibitor MTB-9655 selectively targets, binds to and inhibits the activity of ACSS2. This prevents acetate metabolism to acetyl-CoA which may lead to an inhibition of tumor cell proliferation. ACSS2, an enzyme that converts acetate to acetyl-CoA, is upregulated in cancer cells in response to low nutrient availability and hypoxia. Stressed cancer cells utilize acetate as an alternative nutrient source for cell growth.