Uses
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
Definition
ChEBI: [5-fluoro-1-(4-isopropylbenzylidene)-2-methylinden-3-yl]acetic acid is a sulindac-based non-steroidal anti-inflammatory drug. It has a role as a non-steroidal anti-inflammatory drug. It is functionally related to an acetic acid.
in vivo
K-80003 is a potent inhibitor of AKT activation by all-trans-retinoic acid. K-80003 displays enhanced efficacy in inhibiting tRXRα-dependent AKT activation and tRXRα tumor growth in animals. K-80003 has high affinity to RXRα but lacks COX inhibitory activity[1].
References
[1] Zhou H, et al. NSAID sulindac and its analog bind RXRalpha and inhibit RXRalpha-dependent AKT signaling. Cancer Cell. 2010 Jun 15;17(6):560-73. DOI:
10.1016/j.ccr.2010.04.023[2] Chen L, et al. Modulation of nongenomic activation of PI3K signalling by tetramerization of N-terminally-cleaved RXRα. Nat Commun. 2017 Jul 17;8:16066. DOI:
10.1038/ncomms16066
