| 產(chǎn)品描述： | GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM. |
| 靶點(diǎn)： |
IC50: 4 nM (EZH2), 240 nM (EZH1);HistoneMethyltransferase;?Autophagy |
| 體內(nèi)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 |
| 參考文獻(xiàn)： |
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) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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