WK500B is an orally available small molecule BCL6 inhibitor with IC50 of 1.39 uM (HTFR), exhibits potent efficacy against DLBCL in vitro and in vivo.
WK500B engaged BCL6 inside cells, blocked BCL6 repression complexes, reactivated BCL6 target genes, killed DLBCL cells and caused apoptosis as well as cell cycle arrest.
WK500B inhibited germinal center (GC) formation and DLBCL tumour growth without toxic and side effects in animal models.
WK500B displayed strong efficacy and favourable pharmacokinetics and presented superior druggability.
