ZLD115 is a potent, selective inhibitor of fat mass and obesity-associated protein (FTO) with IC50 of 2.3 uM in PAGE-based assays.
ZLD115 inhibitsFTO demethylase by more than 70% at a concentration of 20 μM, does not inhibit the in vitro demethylation activity of ALKBH3 and ALKBH5 even at a concentration of 200 μM.
ZLD115 exhibits antiproliferative activity in leukemia cell lines MOLM13 and NB4 with IC50 of 1.7 μM and 1.5 μM respectively.
ZLD115 exhibits considerable antiproliferative effects on leukemia cell lines, such as HEL, KG-1, MV-4-11, and THP-1 cell lines, in addition to MOLM13 and NB4 AML cell lines, with IC50 values of 10.3 ± 0.6, 4.1 ± 0.5, 3.4 ± 0.1, and 6.0 ± 1.8 μM, respectively.
ZLD115 (5-10 uM) results in RARA upregulation and MYC downregulation, increases the RARA protein levels in the MOLM13 cells but decreases the abundance of MYC protein.
ZLD115 (40 mg/kg) inhibits leukemia progressionxenograft mouse model by subcutaneously inoculating MV-4-11 cells into female BALB/c nude mice.