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].
Molecular Weight:
374.45
Purity:
99.46
CAS Number:
[1346513-17-4]
Formula:
C23H23FN4
Target:
Akt,Apoptosis,PI3K,RAR/RXR
Application Notes:
MCE Product type: Reference compound1
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