| Identification | Back Directory | [Name]
()-AS 115 | [CAS]
926657-43-4 | [Synonyms]
()-AS 115
BTYYXSHZANWPEB-ZWKOTPCHSA-N
Carbamic acid, N-[2-[[(1R,2S)-2-(butoxymethyl)cyclohexyl]methoxy]ethyl]-, 2-fluorophenyl ester, rel- | [Molecular Formula]
C21H32FNO4 | [MOL File]
926657-43-4.mol | [Molecular Weight]
381.48 |
| Hazard Information | Back Directory | [Description]
KIAA1363 is a 2-acetyl monoacylglyceryl ether (MAGE) hydrolase that is upregulated in aggressive cancers from various tissues.1 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.2 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 SKOV3.2 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. | [Uses]
AS115 is a potent and selective KIAA1363 inactivator with IC50 value of 150 nM. KIAA1363 is a 2-acetyl monoacylglycerol ether (MAGE) hydrolase that is upregulated in aggressive cancers of various tissues[1][2]. | [References]
1. Jessani, N., Liu, Y., Humphrey, M., et al. Enzyme activity profiles of the secreted and membrane proteome that depict cancer cell invasiveness Proc. Natl. Acad. Sci. USA 99(16),10335-10340(2002).
2. Chiang, K.P., Niessen, S., Saghatelian, A., et al. An enzyme that regulates ether lipid signaling pathways in cancer annotated by multidimensional profiling Chem. Biol. 13(10),1041-1050(2006). |
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