ITF 2357

ITF 2357 is an inhibitor of class I and class II histone deacetylases (HDACs).¹ It inhibits HDAC1, -2, -3, -4, -6, and -7 in a fluorometric assay using a baculoviral system expressing the recombinant human isoforms (EC₅₀s = 28, 56, 21, 52, 27, and 163 nM, respectively). ITF 2357 (0.2 µM) reduces the viability of Raji, NAMALWA, SU-DHL-4, and DoHH2 c-Myc⁺ B cell non-Hodgkin lymphoma (NHL) cells, as well as reduces the expression of c-Myc and induces apoptosis in the same cells.² It reduces tumor volume in Raji or NAMALWA mouse xenograft models when administered alone at a dose of 50 mg/kg, with an additive effect when administered in combination with cyclophosphamide (Item No. 13849). ITF 2357 decreases LPS-induced secretion of TNF-α, IL-1α, IL-1β, and IFN-γ in primary human peripheral blood mononuclear cells (PBMCs).³ It also reduces LPS-induced increases in serum Tnf-α and Ifn-γ in mice when administered at doses ranging from 1 to 10 mg/kg. Formulations containing ITF 2357 have been used in the treatment of Duchenne muscular dystrophy (DMD).

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1. Khan, N., Jeffers, M., Kumar, S., et al. Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. Biochem. J. 409(2), 581-589 (2008).

2. Zappasodi, R., Cavanè, A., Iorio, M.V., et al. Pleiotropic antitumor effects of the pan-HDAC inhibitor ITF2357 against c-Myc-overexpressing human B-cell non-Hodgkin lymphomas. Int. J. Cancer 135(9), 2034-2045 (2014).

3. Leoni, F., Fossati, G., Lewis, E.C., et al. The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo. Mol. Med. 11(1-12), 1-15 (2005).