| 产品描述: | ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis. |
| 靶点: |
Histone Methyltransferase |
| 体外研究: |
ZLD1039 inhibited the H3K27me3 and H3K27me2 levels in MCF-7 (0.25~2 μM, 4 days) and MDA-MB-231 (1~4 μM, 4 days) cells in a dose-dependent manner |
| 参考文献: |
1. Xuejiao Song, et al. Selective inhibition of EZH2 by ZLD1039 blocks H3K27methylation and leads to potent anti-tumor activity in breast cancer. Sci Rep. 2016; 6: 20864. 2. Song X, Gao T, Wang N, Feng Q, You X, Ye T, Lei Q, Zhu Y, Xiong M, Xia Y, Yang F, Shi Y, Wei Y, Zhang L, Yu L. Selective inhibition of EZH2 by ZLD1039 blocks H3K27 methylation and leads to potent anti-tumor activity in breast cancer. Sci Rep. 2016 Feb 12;6:20864. doi: 10.1038/srep20864. PubMed PMID: 26868841; PubMed Central PMCID: PMC4751454. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.632 ml |
8.159 ml |
16.318 ml |
| 5 mM |
0.326 ml |
1.632 ml |
3.264 ml |
| 10 mM |
0.163 ml |
0.816 ml |
1.632 ml |
| 50 mM |
0.033 ml |
0.163 ml |
0.326 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。 |