產品描述: | TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4 |
靶點: |
IC50: 134 nM (CBP); 5.02 μM (BRD4);EpigeneticReaderDomain |
體外研究: |
Exposure to 1 μM TPOP146 results in a significant decrease of recovery half-life that is comparable to the construct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146 targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments |
參考文獻: |
1. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.076 ml |
10.382 ml |
20.765 ml |
5 mM |
0.415 ml |
2.076 ml |
4.153 ml |
10 mM |
0.208 ml |
1.038 ml |
2.076 ml |
50 mM |
0.042 ml |
0.208 ml |
0.415 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。 |