Catalog No.: PC-22677Not For Human Use, Lab Use Only.
DDO-2728 is a selective, 2-OG independent inhibitor of mRNA m6A demethylase AlkB homologue 5 (ALKBH5) with IC50 of 2.97 uM in FP assays, does not inhibit FTO (ALKBH9) and ALKBH3.
DDO-2728 is a selective, 2-OG independent inhibitor of mRNA m6A demethylase AlkB homologue 5 (ALKBH5) with IC50 of 2.97 uM in FP assays, does not inhibit FTO (ALKBH9) and ALKBH3.
DDO-2728 directly binds to ALKBH5 with KD of 6.62 uM, but not FTO.
DDO-2728 does not bind to the 2-OG pocket.
DDO-2728 increases m6A methylation levels in the MOLM-13 cells and exhibits antiproliferation activity in AML cells with IC50 of 0.45 and 1.2 uM for MOLM-13 and MV4–11 cells respectivey.
DDO-2728 targets ALKBH5-TACC3 signaling axis, significantly reduces the abundance of TACC3 and c-Myc at both the mRNA and protein levels in MOLM-13 and MV4–11 cells.
DDO-2728 (10 mg/kg, i.p.) significantly inhibited tumor growth in MV4–11 xenograft tumor model.
