Dimethylamino Parthenolide

Dimethylamino parthenolide (DMAPT) is an inhibitor of NF-kappaB and a derivative of parthenolide (Cay-70080). It inhibits the binding of the p65 subunit of NF-kappaB 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 (Cay-20261), NADPH oxidase inhibitor apocynin (Cay-11976), or RIP1 kinase inhibitor necrostatin-1 (Cay-11658). DMAPT (50 mg/kg) decreases tumor volume in an MDA-MB-231 mouse xenograft model.Formal Name: (1aR,4E,7aS,8R,10aS,10bR)-8-[(dimethylamino)methyl]-2,3,6,7,7a,8,10a,10b-octahydro-1a,5-dimethyl-oxireno[9,10]cyclodeca[1,2-b]furan-9(1aH)-one. CAS Number: 791595-09-0. Synonyms: DMAPT, LC-1. Molecular Formula: C17H27NO3. Formula Weight: 293.4. Purity: >99%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: Miscible, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: Miscible, Ethanol: 30 mg/ml. SMILES: O=C([C@H]1CN(C)C)O[C@@]2([H])[C@@]1([H])CC/C(C)=C\CC[C@]3(C)[C@@H]2O3. InChi Code: InChI=1S/C17H27NO3/c1-11-6-5-9-17(2)15(21-17)14-12(8-7-11)13(10-18(3)4)16(19)20-14/h6,12-15H,5,7-10H2,1-4H3/b11-6-/t12-,13-,14-,15+,17+/m0/s1. InChi Key: UJNSFDHVIBGEJZ-WCOQXKCFSA-N.