SAHA-OH, a selective HDAC6 inhibitor with an IC50 of 23 nM, exhibits a 10- to 47-fold greater selectivity for HDAC6 over HDACs 1, 2, 3, and 8. It demonstrates anti-inflammatory effects and reduces macrophage apoptosis [1].

HDAC6:23 nM, HDAC1:237 nM, HDAC3:359 nM, HDAC2:399 nM, HDAC8:1070 nM

SAHA-OH, at concentrations ranging from 0.67 to 10.76 μM over a period of 51 hours, demonstrates inhibitory effects on bone marrow macrophages [1]. When applied to bone marrow-derived macrophages (BMMØs) at 0.01 μM for 3 hours, SAHA-OH significantly reduces the secretion of cytokines such as IL-6, TNFα, IFNβ, IL-1β, IL-10, MCP-1 (CCL2), and GROα (CXCL1) [1]. Additionally, a 10 μM SAHA-OH treatment for either 4 or 9 hours results in increased acetylation of cytoplasmic α-tubulin and nuclear histone H3 [1]. At dosages up to 30 μM, a 3-hour treatment with SAHA-OH effectively decreases apoptosis in macrophages and reduces death in B cells [1].

SAHA-OH, administered through intraperitoneal injection at a dose of 50 mg/kg in a single dose, mitigates splenic damage and diminishes the levels of proinflammatory cytokines in plasma in a mouse model of LPS-induced endotoxemia [1].