Dimethylamino parthenolide (DMAPT) is an inhibitor of NF-κB and a derivative of parthenolide .1 It inhibits the binding of the p65 subunit of NF-κB to DNA by 75% when used at a concentration of 50 µM. DMAPT (25 µM) decreases intracellular glutathione (GSH) levels in, and inhibits the migration of, MDA-MB-231 breast cancer cells. It induces necrosis in MDA-MB-231 cells, an effect that can be reversed by the antioxidant N-acetyl cysteine , NADPH oxidase inhibitor apocynin , or RIP1 kinase inhibitor necrostatin-1 . DMAPT (50 mg/kg) decreases tumor volume in an MDA-MB-231 mouse xenograft model.
1.D'Anneo, A., Carlisi, D., Lauricella, M., et al.Parthenolide generates reactive oxygen species and autophagy in MDA-MB231 cells. A soluble parthenolide analogue inhibits tumour growth and metastasis in a xenograft model of breast cancerCell Death Dis.4(e891)(2013)