K-8012 is a potent RXRa antagonist, with an IC50 of approximately 9.2 μM for inhibiting 9-cis-retinoic acid-induced Gal4-RXRa-LBD trans-activation. This compound demonstrates enhanced anticancer activity compared to sulindac in an RXRa-dependent manner. K-8012 effectively inhibits the tRXRa-mediated PI3K/AKT signaling pathway, promoting apoptosis and suppressing AKT activation by disrupting the interaction between tRXRa and p85α. These properties make K-8012 valuable for research in cancer biology and signaling pathways.
K-8012 is a potent RXRa antagonist, with an IC50 of approximately 9.2 μM for inhibiting 9-cis-retinoic acid-induced Gal4-RXRa-LBD trans-activation. This compound demonstrates enhanced anticancer activity compared to sulindac in an RXRa-dependent manner. K-8012 effectively inhibits the tRXRa-mediated PI3K/AKT signaling pathway, promoting apoptosis and suppressing AKT activation by disrupting the interaction between tRXRa and p85α. These properties make K-8012 valuable for research in cancer biology and signaling pathways.
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