Bufexamac

Bufexamac is an NSAID and inhibitor of the class IIb histone deacetylases HDAC6 and HDAC10.¹ It inhibits the production of IFN-α in peripheral blood mononuclear cells (PBMCs; EC₅₀ = 8.9 µM). Bufexamac induces hyperacetylation of tubulin (IC₅₀ = 2.9 µM), a major substrate of HDAC6, without increasing acetylation of the class I HDAC substrates H3K5 or H3K9/K14. It also inhibits leukotriene A₄ (LTA₄) hydrolase and aminopeptidase activity (IC₅₀s = 15.86 and 11.59 µM, respectively) and 5-lipoxygenase (5-LO) activity (IC₅₀ = 27 µM).^2,3 Bufexamac inhibits the production of leukotriene B₄ (LTB₄; Item No. 20110) in neutrophils (IC₅₀ = 12.91 µM) and reduces fMLP-induced neutrophil migration when used at concentrations of 50 and 100 µM.² It also reduces neutrophil levels, as well as protein levels of TNF-α and IL-1β, in bronchoalveolar lavage fluid (BALF) in a mouse model of LPS-induced acute lung injury when administered at a dose of 100 mg/kg.

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1. Bantscheff, M., Hopf, C., Savitski, M.M., et al. Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes. Nat. Biotechnol. 29(3), 255-265 (2011).

2. Xiao, Q., Dong, N., Yao, X., et al. Bufexamac ameliorates LPS-induced acute lung injury in mice by targeting LTA₄H. Sci. Rep. 6:25298, (2016).

3. Summers, J.B., Kim, K.H., Mazdiyasni, H., et al. Hydroxamic acid inhibitors of 5-lipoxygenase: quantitative structure-activity relationships. J. Med. Chem. 33(3), 992-998 (1990).