| Description | DMAPT (Dimethylamino Parthenolide) is a water-soluble analogue of Parthenolide (PTL). It is an orally active NF-κB inhibitor with an LD50 of 1.7 μM on primary acute myeloid leukemia cells. |
| In vitro | DMAPT处理降低了NF-κB的固有结合活性，并抑制了PC-3和DU145细胞的增殖与存活率。PC-3和DU145细胞分别用5和4μM的DMAPT处理，导致PC-3前列腺癌细胞的倍增时间从23.0±5.0小时增加到42.0±3.0小时，而DU145细胞的倍增时间则从20.4±2.2小时增长至72.5±24.8小时。 |
| In vivo | DMAPT（每日口腔灌胃，100 mg/kg，连续7天）处理能提高PC-3肿瘤异种移植物对X射线的敏感性。DMAPT（从出生后的42至300天，每周三次口腔灌胃，100 mg/kg）处理可延缓TRAMP小鼠正常肿瘤的发展，并将可触及的前列腺肿瘤时间延长20%。此外，DMAPT还将TRAMP小鼠的肺组织转移区域减少到低于水载体处理组（0.10%±0.15 SD，降低了92%，p = 0.0028）[3]。 |
| Target activity | NF-κB:1.7 μM(LD50) |
| Synonyms | Dimethylamino Parthenolide |
| molecular weight | 293.4 |
| Molecular formula | C17H27NO3 |
| CAS | 870677-05-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (340.83 mM), Sonication is recommended. |
| References | 1. Neelakantan S, et al. Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-kappaB inhibitor, DMAPT (LC-1). Bioorg Med Chem Lett. 2009 Aug 1;19(15):4346-9. 2. Mendonca MS, et al. DMAPT inhibits NF-κB activity and increases sensitivity of prostate cancer cells to X-rays in vitro and in tumor xenografts in vivo. Free Radic Biol Med. 2017 Nov;112:318-326. 3. Morel KL, et al. Chronic low dose ethanol induces an aggressive metastatic phenotype in TRAMP mice, which is counteracted by parthenolide. Clin Exp Metastasis. 2018 Oct;35(7):649-661. |