Catalog No.: PC-73322Not For Human Use, Lab Use Only.
EZM 0414 is a potent, selective and orally bioavailable inhibitor of histone methyltransferase SETD2 with biochemical IC50 of 18 nM, >10,000-fold selectivity over other HMTases.
EZM 0414 is a potent, selective and orally bioavailable inhibitor of histone methyltransferase SETD2 with biochemical IC50 of 18 nM, >10,000-fold selectivity over other HMTases.
EZM 0414 reduced global tri-methylation of H3K36 (H3K36me3, IC50=34 nM) in t(4;14) bearing MM cell lines, with no effect on global di-methyl H3K36 (H3K36me2) levels.
EZM 0414 demonstrated broad anti-proliferative effects of EZM0414 in a panel of MM cell lines with enhanced sensitivity in cells harboring the (4;14) chromosomal translocation, as well as in a panel of DLBCL cell lines representing both GCB and ABC subtypes.
EZM 0414 suppressed tumor volume and inhibited H3K36me3 level in human MM and DLBCL xenograft models.
