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Description: ML349 is a novel, potent, reversible, highly selective and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM. Although ML349 is highly selective within the serine hydrolase enzyme family, it could still interact with other cellular targets. In human cell lysates, biotinylated-ML349 enriches a recurring set of proteins, including metabolite kinases and flavin-dependent oxidoreductases that are potentially enhanced by avidity-driven multimeric interactions. ML349 achieves target engagement and hydrolase selectivity in living mice.
References: Oncotarget. 2016 Feb 9; 7(6):7297-306.; ACS Chem Biol. 2016 Dec 16; 11(12):3374-3382.
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