References: |
MC3343 (MC-3343) is a novel potent, non-nucleoside DNA methyltransferase (DNMT) inhibitor with IC50 of 5.7 and 1.7 uM for DNMT1 and DNMT3a in cell-free assays, respectively; displays increased potency against DNMT1 compared with RG-108 and SGI-1027; efficiently inhibits OS cell proliferation and induces osteoblastic differentiation, induces dose- and time-dependent decreases in DNMT1, DNMT3a and DNMT3b protein levels in Saos-2 OS cells; displays synergistic effects with doxorubicin and cisplatin in vivo, reduces patient-derived xenograft OS growth and induces differentiation. |