METTL3 inhibitor UZH2 is a potent, selective and cell-permeable RNA methyltransferase METTL3 inhibitor with IC50 of 5 nM in TR-FRET assays.
UZH2 displays no affinity against METTL16 and METTL1 in a thermal shift assay at 100 uM.
UZH2 dose-dependently decreased MOLM-13 and PC-3 cell growth following 72 h of incubation, with GI50 values of 12 and 70 μM, respectively.
UZH2 dose-dependently stabilize METTL3, with EC50 values of 2 and 0.85 μM in HEK293T cells and AML MOLM-13 cells through the InCELL Pulse assay and CETSA, respectively.
UZH2 reduced the m6A/A level of polyadenylated RNA in MOLM-13 (acute myeloid leukemia) and PC-3 (prostate cancer) cell lines.
