| Identification | Back Directory | [Name]
2H-Tetrazole, 5-[2-[(1Z)-5-fluoro-2-methyl-1-[[4-(1-methylethyl)phenyl]methylene]-1H-inden-3-yl]ethyl]- | [CAS]
1346513-17-4 | [Synonyms]
K8012
K-8012
K 8012
2H-Tetrazole, 5-[2-[(1Z)-5-fluoro-2-methyl-1-[[4-(1-methylethyl)phenyl]methylene]-1H-inden-3-yl]ethyl]- | [Molecular Formula]
C23H23FN4 | [MOL File]
1346513-17-4.mol | [Molecular Weight]
374.45 |
| Chemical Properties | Back Directory | [Boiling point ]
549.4±60.0 °C(Predicted) | [density ]
1.223±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
4.94±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
K-8012 is an inhibitor of the interaction of the N-terminally truncated RXR. | [Uses]
K-8012, a sulindac (HY-B0008) analog, is a potent antagonist of RXRa. The IC50 value for K-8012 to inhibit 9-cis-RA-induced Gal4-RXRa-LBD trans-activation were about 9.2 μM. K-8012 exerts improved anticancer activity over sulindac in a RXRa-dependent manner. K-8012 exhibits activity in inhibiting the tRXRa-mediated PI3K/AKT signaling pathway. K-8012 induces apoptosis and inhibits AKT activation by preventing tRXRa from binding to p85a[1]. | [IC 50]
RXR α | [References]
[1] Chen L, et al. Sulindac-derived RXRα modulators inhibit cancer cell growth by binding to a novel site. Chem Biol. 2014 May 22;21(5):596-607. DOI:10.1016/j.chembiol.2014.02.017 |
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