Me-Indoxam

Me-Indoxam is a potent and cell-impermeable secreted phospholipase A₂ (sPLA₂) inhibitor^[1]. IC50 & Target:sPLA₂^[1] In Vitro:Me-Indoxam shows different potencies on the various sPLA₂ isoforms in in vitro assays with an IC₅₀ of less than 100 nM for hGIIA, hGIIE, and hGV; an IC₅₀ of between 200 and 600 nM for hGIB and hGX; and an IC₅₀ of greater than 2 mM for hGIID, hGIIF, hGIII, and hGXIIA^[1].
Me-Indoxam is able to inhibit the activity of sPLA₂s only when they are secreted in the extracellular space^[1].
Me-Indoxam (0-10 μM; 30 min) inhibits Leukotriene C₄ (LTC₄) production from anti-IgE–stimulated primary human lung mast cells (HLMCs)^[1].
Me-indoxam (0.01–10 M) did not affect the basal secretion of TNF-α and IL-6 from human lung macrophages (HLM). Preincubation (15 min, 37°C) of hGX (1 μg/mL) with various concentrations of Me-indoxam before the addition to HLM dose-dependently inhibited TNF-α and IL-6 release. The IC₅₀ values of Me-indoxam were 253±72 and 320±87 nM on TNF-α and IL-6 release, respectively^[2].