DMAPT (Dimethylamino Parthenolide) is an orally active NF-κB inhibitor and a Parthenolide (PTL) analogue with an LD50 value of 1.7 μM for primary acute myeloid leukemia cells. It has potential anti-tumor and anti-metastatic effects.

NF-κB:1.7 μM(LD50)

DMAPT treatment reduced the constitutive NF-κB binding activity and inhibited the proliferation and viability of PC-3 and DU145 cells. Treatment of PC-3 and DU145 cells with 5 and 4 μM DMAPT, respectively, increased the population doubling time of PC-3 prostate cancer cells from 23.0±5.0 h to 42.0±3.0 h, while the population doubling time of DU145 cells increased from 20.4±2.2 h By 72.5±24.8 hours.

DMAPT (100 mg/kg, oral gavage daily for 7 days) treatment can increase the sensitivity of PC-3 tumor xenografts to X-rays. DMAPT (100 mg/kg, 42 to 300 days from birth, oral gavage three times a week) treatment can slow the normal tumor development of TRAMP mice and prolong the reachable prostate tumor time by 20%. DMAPT further reduced the lung tissue transfer area of TRAMP mice to below the water vehicle treatment group (0.10%±0.15 SD, 92% reduction, p = 0.0028)[3].