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**Dimethylaminoparthenolide** is a water-soluble synthetic analog of parthenolide, a natural sesquiterpene lactone, developed for increased solubility and bioavailability over parthenolide[1][3][5][9]. It exhibits broad **anticancer activity** in preclinical models of lung cancer, bladder cancer, pancreatic cancer, chronic myeloid leukemia, acute myeloid leukemia, and triple-negative breast cancer[1][2][3][4][5][6][9]. Its mechanism centers on **inhibition of Nuclear factor kappa-light-chain enhancer of activated B cells (NF-κB)**, leading to reduced tumor cell proliferation, induction of apoptosis, blocked double-stranded DNA break repair, and decreased activity of STAT3 and MCL-1[1][3][5][6][7][9]. DMAPT also increases **reactive oxygen species (ROS)** in cancer cells, depletes glutathione, and thus enhances susceptibility to oxidative stress-induced cell death[2][5][9]. It suppresses inflammatory pathways by inhibiting targets such as NLRP3, Caspase-1, IL-1β, and IL-18[7]. DMAPT has shown clinical potential for **hematological malignancies** with good PK/PD and tolerability in early phase human studies[8].
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