Biological Activity |
FW1256 is a phenyl analogue and a slow-releasing hydrogen sulfide (H2S) donor. FW1256 inhibits NF-kappaB activity and induces cell apoptosis. FW1256 exerts potent anti-inflammatory effects and has the potential for cancer and cardiovascular disease treatment[1][2]. In Vitro: FW1256 (200 uM; 24.5 hours; AW264.7 cells) treatment significantly reduces IL-1beta, COX-2 and iNOS mRNA and protein in LPS-stimulated RAW264.7 macrophages[1]. FW1256 (200 uM; 24.5 hours; AW264.7 cells) treatment significantly reduces IL-1beta, COX-2 and iNOS PROTE and protein in LPS-stimulated RAW264.7 macrophages[1]. FW1256 concentration dependently decreases TNF-alpha (IC50 of 61.2 uM), IL-6 (IC50 of 11.7 uM), PGE2 (IC50 of 25.5 uM) and NO (IC50 of 34.6 uM) generation in LPS-stimulated RAW264.7 macrophages and bone marrow-derived macrophages (BMDMs) (IC50s of 414.9 uM, 300.2 uM, 4 uM and 9.5 uM for TNF-alpha, IL-6, PGE2 and NO, respectively) [1]. FW1256 decreases NF-kappaB activation as evidenced by reduced cytosolic phospho-IkappaBalpha levels and reduces nuclear p65 levels in LPS-stimulated RAW264.7 macrophages treated with FW1256[1]. In Vivo: FW1256 (100 mg/kg; intraperitoneal injection; male C57BL/6 mice) treatment reduces IL-1beta, TNFalpha, nitrate/nitrite and PGE2 levels in LPS-treated mice[1]. |