CBP/p300-IN-12 |
Catalog No.GC64696 |
CBP/p300-IN-12는 강력하고 선택적인 공유 히스톤 아세틸트랜스퍼라제 p300(IC50 166nM) 및 CBP 억제제입니다. CBP/p300-IN-12는 PC-3 세포의 H3K27Ac 수준을 감소시킵니다(37 nM의 EC50). CBP/p300-IN-12는 C1450과 공유 부가물을 형성합니다.
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Cas No.: 2738688-57-6
Sample solution is provided at 25 µL, 10mM.
CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450[1].
CBP/p300-IN-12 (Compound 2) shows antiproliferative effect against androgen receptor (AR)-positive LnCaP-FGC cells (EC50 of 87 nM), while displaying significantly less activity in the AR-negative cell line DU-145 (EC50 of 1.37 μM).
[1]. Anthony Mastracchio, et al. Discovery of a Potent and Selective Covalent p300/CBP Inhibitor. ACS Med Chem Lett. 2021 Apr 5;12(5):726-731.
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