UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor with an IC50 of 280 nM, while UZH1b (IC50=28 μM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes, has antitumor activity, and serves as a chemical probe for studying METTL3[1].

UZH1a (2.5-160 μM; 72 h) inhibits the growth of MOLM-13, HEK293T, and U2Os cells, with IC50s of 11 μM, 67 μM, and 87 μM, respectively. UZH1b (2.5-160 μM; 72 h) inhibits the growth of the same cells, with IC50s of 78 μM, 79 μM, and 93 μM, respectively[1]. UZH1a (2.5-100 μM; 16 h) reduces m6A methylation levels in mRNA from cells dose-dependently (IC50=4.6 μM), whereas UZH1b is less active at concentrations up to 100 μM in MOLM-13 cells. UZH1a (40 μM; 16 h) reduces m6A methylation levels in mRNA from MOLM-13, HEK293T, and U2Os cells. Furthermore, UZH1a (20 μM; 16 h) increases apoptosis and induces cell cycle arrest in MOLM-13 cells[1].