FB23-2

FB23-2 is a potent and selective small molecule inhibitor of FTO, an mRNA N6-methyladenosine (m6A) demethylase implicated in oncogenesis and aberrant epigenetic regulation. FB23-2 was developed using structure-based rational design and directly binds to FTO, selectively inhibiting its demethylase activity (IC50 ~2.6 μM). In preclinical models, FB23-2 suppresses proliferation and promotes differentiation/apoptosis of human acute myeloid leukemia (AML) cell lines and primary AML cells, and shows efficacy in xenografted mice. Its primary mechanism of action is the elevation of m6A methylation in mRNA via FTO inhibition, affecting cell proliferation and survival pathways. Recent studies report that FB23-2 also acts as an off-target inhibitor of human dihydroorotate dehydrogenase (hDHODH), disrupting pyrimidine synthesis, which is implicated in its antiproliferative effects. Additional therapeutic potential has been shown in diabetic retinopathy (by regulating endothelial cell states) and clear cell renal cell carcinoma models[1][2][3][4][5].

Other names

FB23-2FB-23-2FB 23-2