TPOP146 |
| رقم الكتالوجGC32880 |
TPOP146 هو مثبط انتقائي CBP / P300 benzoxazepine bromodomain بقيم 134 نانومتر و 5.02 ميكرومتر لـ CBP و BRD4
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2018300-62-2
Sample solution is provided at 25 µL, 10mM.
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TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
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[1].
[1]. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912.
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