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编 号:F747866
分子式:C17H19ClN2O
分子量:302.8
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生物活性:
PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer.

体外研究:
PBRM1-BD2-IN-1 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibit growth of a PBRM1-dependent prostate cancer cell line.PBRM1-BD2-IN-1 has binding affinity for PBRM1-BD2, PBRM1-BD5, SMARCA2B amd SMARCA4 with Kd values of 0.7 μM, 0.35 μM, 8.1 μM and 5.0 μM, respectively.PBRM1-BD2-IN-1 has inhibitory activity for PBRM1-BD2 with IC50 value of 0.2 μM.
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