tcsc0045 TPCA-1

TPCA-1 is a potent and selective inhibitor of IKK-2 with IC₅₀ of 17.9 nM.

IC50 & Target: IC50: 17.9 nM (IKK)

In Vitro: TPCA-1 significantly represses pro-inflammatory cytokines IL-8 and GRO-α in NPECs^[1]. TPCA-1 inhibit NFκB activity as well as glioma cell proliferation and IL8 expression, and at concentrations of 2.5 and 5 μM, it blocks the TNF-induced p65 translocation into the nucleus of U87 cells^[2]. TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-α, IL-6, and IL-8 with an IC₅₀=170 to 320 nM^[3].

In Vivo: TPCA-1 (3, 10, or 20 mg/kg, i.p.) results in a dose-dependent reduction in the severity of murine collagen-induced arthritis (CIA). TPCA-1 (10 mg/kg, i.p., b.i.d.) in vivo results in significantly decreased collagen-induced T cell proliferation ex vivo^[3].