FB23 is a potent and selective inhibitor of FTO demethylase with IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity.
FB23 is a potent and selective inhibitor of FTO demethylase with IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity.
FB23 treatment inhibits acute myeloid leukemia (AML) cells proliferation with IC50 values of 44.8 μM, 23.6 μM for NB4 and MONOMAC6 AML cells. FB23 treatment causes the significant suppression of MYC targets, E2F targets, and G2M checkpoint signal cascades, which may contribute to the inhibitory effects of FTO inhibitors and FTO KD on cell cycle and proliferation. FB23 treatments activates apoptosis and p53 pathways.[1]
Pharmacological inhibition of FTO by FB23-2 substantially suppresses leukemia progression and prolongs survival.[1]
[1] Yue Huang, et al. Cancer Cell. 2019 Apr 15;35(4):677-691.e10.
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