wp631

WP631 is a **bisanthracycline derivative** of daunorubicin (daunomycin), designed as a **bisintercalating anthracycline** that binds strongly to DNA by occupying six base pairs, compared to three by monointercalators[1][3]. It acts primarily as a **potent inhibitor of Sp1-activated transcription**, blocking basal and especially Sp1-activated initiation by **preventing binding of Sp1 transcription factor to its GC-rich DNA binding site**[1][3]. WP631 shows a high affinity for CpG-rich DNA elements, displacing transcription factors and effectively reducing transcription from promoters with Sp1 sites. It is much more efficient than daunomycin at this mechanism[1]. WP631 can induce **caspase-dependent apoptosis** in human cancer cells and synergizes with drugs such as epothilone B (Epo B) in increasing apoptosis and DNA damage in cancer models, especially ovarian cancer[2][4]. WP631 has also been shown to inhibit HIV-1 replication by blocking Tat-dependent transactivation[3]. The compound is primarily used in research and is not approved for clinical use[3].

Other names

4-Methylbenzyl-N-bis[daunomycin], mesylate saltbisanthracycline WP631