| 产品描述: | CDDO-Im (RTA-403) is an activator of Nrf2 and PPAR, with Kis of 232 and 344 nM for PPARα and PPARγ |
| 靶点: |
PPARα:232 nM (Ki);PPARγ:344 nM (Ki);Nrf2;Ferroptosis;Nrf2;PPAR |
| 体外研究: |
CDDO-Im is highly active in suppressing cellular proliferation of human leukemia and breast cancer cell lines (IC50 approximately 10-30 nM). In U937 leukemia cells, CDDO-Im also induces monocytic differentiation as measured by increased cell surface expression of CD11b and CD36. Treatment with CDDO-Im elevates protein levels of Nrf2, a transcription factor previously shown to bind ARE sequences, and increases expression of a number of antioxidant and detoxification genes regulated by Nrf2. CDDO-Im is one of the most potent synthetic triterpenoids shown to induce growth inhibition and apoptosis in various human cancer cells, including multiple myeloma, lung, pancreas and breast cancer. CDDO-Im treatment markedly induces cell cycle arrest at G2/M-phase and apoptosis in the triple-negative breast cancer cell lines, SUM159 and MDA-MB-231. The CD24−/EpCAM+ cells in SUM159 tumorspheres are significantly inhibited by CDDO-Im treatment. CDDO-Im also significantly decreases sphere forming efficiency and tumorsphere size in both primary and secondary sphere cultures. |
| 体内研究: |
CDDO-Im is a potent inhibitor of de novo inducible nitric oxide synthase expression in primary mouse macrophages. Moreover, CDDO-Im inhibits growth of B16 murine melanoma and L1210 murine leukemia cells in vivo. Injection of 10 nM (5.4 μg) of CDDO-Im almost completely blocks the ability of IFN-γ to induce iNOS, and treatment with as little as 1 nmol of CDDO-Im (0.54 μg) is partially effective. |
| 参考文献: |
1. Place AE, et al. The novel synthetic triterpenoid, CDDO-imidazolide, inhibits inflammatory response and tumor growth in vivo. Clin Cancer Res. 2003 Jul;9(7):2798-806. 2. Liby K, et al. The synthetic triterpenoids, CDDO and CDDO-imidazolide, are potent inducers of heme oxygenase-1 and Nrf2/ARE signaling. Cancer Res. 2005 Jun 1;65(11):4789-98. 3. So JY, et al. A synthetic triterpenoid CDDO-Im inhibits tumorsphere formation by regulating stem cell signaling pathways in triple-negative breast cancer. PLoS One. 2014 Sep 17;9(9):e107616. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.846 ml |
9.23 ml |
18.46 ml |
| 5 mM |
0.369 ml |
1.846 ml |
3.692 ml |
| 10 mM |
0.185 ml |
0.923 ml |
1.846 ml |
| 50 mM |
0.037 ml |
0.185 ml |
0.369 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |