產品描述: | BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 |
靶點: |
G9a:6.3 μM (IC50);PRC2;HistoneMethyltransferase |
體外研究: |
BRD9539 decreases ATP levels in a dose-dependent manner in HeLa cells. BRD9539 is a more potent biochemical inhibitor than its methyl-ester analogue BRD4770, with 20% remaining G9a activity compared to 45% of BRD4770 at screening concentration. However, BRD9539 has no activity in cell-based assays, presumably due to impaired cell permeability compared to that of BRD4770. In addition, the activities of 16 other chromatin-modifying enzymes and 100 kinases involved in cell-cycle regulation and cancer cell biology are tested for activity in the presence of 5 or 10 μM BRD9539; no activity is seen in any of these assays. |
參考文獻: |
1. Yuan, Y., Wang, Q., Paulk, J., et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma ACS Chem. Biol. 7(7), 1152-1157 (2012). |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.503 ml |
12.517 ml |
25.035 ml |
5 mM |
0.501 ml |
2.503 ml |
5.007 ml |
10 mM |
0.25 ml |
1.252 ml |
2.503 ml |
50 mM |
0.05 ml |
0.25 ml |
0.501 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |