产品描述: | GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM. |
靶点: |
IC50: 4 nM (EZH2), 240 nM (EZH1);HistoneMethyltransferase; Autophagy |
体内研究: |
Compare with the controls, GSK343 (5 mg/kg)-treated mice exhibits significantly inhibited tumor growth. The average tumor volume and weight of the GSK343-treated cohort is remarkably reduced. As early as 20 days post-implantation, a significant reduction in tumor growth is observed in the GSK343-treated cohort relative to the control cohort; this difference persisted through the remainder of the study. In addition, compare with the control cohort, the GSK343-treated animals in the xenograft model show a remarkable increase in messenger RNA levels of E-cadherin but a significant decrease in vimentin messenger RNA levels |
参考文献: |
1. Sharad K, et al. Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. 2. Ding M, et al. The polycomb group protein enhancer of zeste 2 is a novel therapeutic target for cervical cancer. Clin Exp Pharmacol Physiol. 2015 May;42(5):458-64. |
溶解性: |
DMSO : 15.62 mg/mL (28.84 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.846 ml |
9.23 ml |
18.461 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。 |