Single enantiomer of a potent inhibitor of a cancer-promoting enzyme
KIAA1363 is a 2-acetyl monoacylglyceryl ether (MAGE) hydrolase that is upregulated in aggressive cancers from various tissues. The enzyme catalyzes the hydrolysis of the 2-acetyl MAGE to MAGE and serves as a central enzyme in the PAF and LPA signaling network. AS 115 is a potent and selective inactivator of KIAA1363, displaying an IC50 value of 150 nM when tested as a racemic mixture in the invasive ovarian cancer cell line SKOV3. Treatment of SKOV3 cells with 10 µM AS-115 for 4 hours significantly reduced the formation of MAGE, alkyl-lysophosphatidylcholine, and alkyl-lysophosphatidic acid. The activity of the individual enantiomers of AS 115, i.e., (+)-AS 115 and (-)-AS 115, has not been determined.
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