FW1256

FW1256 is a phenyl analogue and a slow-releasing hydrogen sulfide (H2S) donor. FW1256 induces cell apoptosis. FW1256 has the potential for cancer, inflammation, and cardiovascular disease treatment[1][2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Research Areas >> Cardiovascular Disease

Research Areas >> Inflammation/Immunology

FW1256 (200 µM; 24.5 hours; AW264.7 cells) treatment significantly reduces IL-1β, COX-2 and iNOS mRNA and protein in LPS-stimulated RAW264.7 macrophages[1]. FW1256 (200 µM; 24.5 hours; AW264.7 cells) treatment significantly reduces IL-1β, COX-2 and iNOS PROTE and protein in LPS-stimulated RAW264.7 macrophages[1]. FW1256 concentration dependently decreases TNF-α (IC50 of 61.2 µM), IL-6 (IC50 of 11.7 µM), PGE2 (IC50 of 25.5 µM) and NO (IC50 of 34.6 µM) generation in LPS-stimulated RAW264.7 macrophages and bone marrow-derived macrophages (BMDMs) (IC50s of 414.9 µM, 300.2 µM, 4 µM and 9.5 µM for TNF-α, IL-6, PGE2 and NO, respectively) [1]. FW1256 decreases NF-κB activation as evidenced by reduced cytosolic phospho-IκBα levels and reduces nuclear p65 levels in LPS-stimulated RAW264.7 macrophages treated with FW1256[1]. RT-PCR[1] Cell Line: RAW264.7 cells Concentration: 200 µM Incubation Time: 24.5 hours Result: Significantly reduced IL-1β, COX-2 and iNOS mRNA in LPS-stimulated RAW264.7 macrophages.. Western Blot Analysis[1] Cell Line: RAW264.7 cells Concentration: 200 µM Incubation Time: 24.5 hours Result: Significantly reduced IL-1β, COX-2 and iNOS proteinin LPS-stimulated RAW264.7 macrophages..

FW1256 (100 mg/kg; intraperitoneal injection; male C57BL/6 mice) treatment reduces IL-1β, TNFα, nitrate/nitrite and PGE2 levels in LPS-treated mice[1]. Animal Model: Male C57BL/6 mice (20-25 g, 6-10 weeks) injected with E. coli lipopolysaccharide (LPS)[1] Dosage: 100 mg/kg Administration: Intraperitoneal injection Result: Reduced IL-1β, TNFα, nitrate/nitrite and PGE2 levels in LPS-treated mice.

[1]. Huang CW, et al. A novel slow-releasing hydrogen sulfide donor, FW1256, exerts anti-inflammatory effects in mouse macrophages and in vivo. Pharmacol Res. 2016 Nov;113(Pt A):533-546.

[2]. Feng W, et al. Discovery of New H2S Releasing Phosphordithioates and 2,3-Dihydro-2-phenyl-2-sulfanylenebenzo[d][1,3,2]oxazaphospholes with Improved Antiproliferative Activity. J Med Chem. 2015 Aug 27;58(16):6456-80.