UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1b (IC50=28 µM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes. UZH1 has antitumor activity. UZH1 also can be used 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[1].UZH1b (2.5-160 µM; 72 h) inhibits the growth of MOLM-13, HEK293T, and U2Os cells, with IC50s of 78 µM, 79 µM, and 93 µM, respectively[1].UZH1a (2.5-100 µM; 16 h) reduces m6A methylation level in mRNA from cells in a dose-dependent manner (IC50=4.6 µM), while UZH1b is less active at concentrations up to 100 µM in MOLM-13 cells[1].UZH1a (40 µM; 16 h) reduces m6A methylation level in mRNA from MOLM-13, HEK293T, and U2Os cells[1].UZH1a (20 µM; 16 h) increases apoptosis and leads to cell cycle arrest in MOLM-13 cells[1].
[1]. Moroz-Omori EV, et, al. METTL3 inhibitors for epitranscriptomic modulation of cellular processes. bioRxiv. 2020 Oct 13.