| Bioactivity | 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]. |
| CAS | 1346513-17-4 |
| Formula | C23H23FN4 |
| Molar Mass | 374.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |