BML-210

BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50 of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice[1][2][3].

[1]Nimanthi Jayathilaka, et al. Inhibition of the function of class IIa HDACs by blocking their interaction with MEF2. Nucleic Acids Res. 2012 Jul; 40(12): 5378–5388.|[2]Veronika Borutinskaite, et al. The Histone Deacetylase Inhibitor BML-210 Influences Gene and Protein Expression in Human Promyelocytic Leukemia NB4 Cells via Epigenetic Reprogramming. Int J Mol Sci. 2015 Aug; 16(8): 18252–18269.|[3]Zhuolong Zhou, et al. An organoid-based screen for epigenetic inhibitors that stimulate antigen presentation and potentiate T-cell-mediated cytotoxicity. Nat Biomed Eng. 2021 Nov;5(11):1320-1335.