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 SK0V-3. Treatment of SKOV-3 cells with 10 uM 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.
產(chǎn)品描述
A single enantiomer of a potent and selective inactivator of KIAA1363, a MAGE hydrolase an enzyme that is upregulated in addressive cancers from various tissues -IC50 = 150 nM when tested as a racemic mixture in SK0V-3 cells); activity of the individual enantiomers of AS 115, i.e. -+)-AS 115 and --)-AS 115, has not been determined