For research use only. Not for therapeutic Use.
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
When MCF-7 cells are cotreated with K-80003, TNFα-induced colocalization of tRXRα with p85α in the cytoplasm is inhibited, resulting in tRXRα nuclear localization. Western blotting shows that K-80003-stabilized tetrameric form of tRXRα is found exclusively in the nuclear fraction, while tRXRα monomer is distributed both in the nuclear and cytoplasmic fractions[2].
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].
| Catalog Number | I012903 |
| CAS Number | 1292821-90-9 |
| Synonyms | 2-[(3Z)-6-fluoro-2-methyl-3-[(4-propan-2-ylphenyl)methylidene]inden-1-yl]acetic acid |
| Molecular Formula | C22H21FO2 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H21FO2/c1-13(2)16-6-4-15(5-7-16)10-19-14(3)20(12-22(24)25)21-11-17(23)8-9-18(19)21/h4-11,13H,12H2,1-3H3,(H,24,25)/b19-10- |
| InChIKey | QCXBVGNDRYQVJO-GRSHGNNSSA-N |
| SMILES | CC1=C(C2=C(C1=CC3=CC=C(C=C3)C(C)C)C=CC(=C2)F)CC(=O)O |
| Reference | [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. [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. |
