| Bioactivity | (S)-DMAPT (Dimethylamino Parthenolide), an analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect[1]. |
| Invitro | DMAPT 处理降低了组成型 NF-κB 结合活性，抑制了 PC-3 和 DU145 细胞的细胞增殖和活力[2]。5 和 4 μM DMAPT 处理 PC-3 和 DU145 细胞，分别将 PC-3 前列腺癌细胞的群体倍增时间从 23.0 ± 5.0 小时增加到 42.0 ± 3.0 小时，将 DU145 细胞的群体倍增时间从 20.4 ± 2.2 小时增加到 72.5 ± 24.8 小时[2]。 0 --> (S)-DMAPT 相关抗体: |
| In Vivo | 用 DMAPT (100 mg/kg，每天口服管饲法，持续 7 天) 处理可提高 PC-3 肿瘤异种移植物对 X 射线的敏感性[2]。 DMAPT (100 mg/kg，从出生后 42 天到 300 天，每周口服管饲三次) 处理可减缓 TRAMP 小鼠的正常肿瘤发展，将可触及前列腺肿瘤的时间延长 20%[3]。 DMAPT 进一步在 TRAMP 小鼠[3]中，肺组织中的转移面积低于水载体处理组 (0.10% ± 0.15 SD，减少 92%，p=0.0028)。 |
| Name | (S)-DMAPT |
| CAS | 870677-05-7 |
| Formula | C17H27NO3 |
| Molar Mass | 293.40 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |