Bioactivity | FW1256 is a phenyl analogue and a slow-releasing hydrogen sulfide (H2S) donor. FW1256 inhibits NF-κB activity and induces cell apoptosis. FW1256 exerts potent anti-inflammatory effects and has the potential for cancer and cardiovascular disease treatment[1][2]. | ||||||||||||
Invitro | 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: | ||||||||||||
In Vivo | 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: | ||||||||||||
Name | FW1256 | ||||||||||||
CAS | 117089-08-4 | ||||||||||||
Formula | C12H10NOPS | ||||||||||||
Molar Mass | 247.25 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |