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编 号:F762598
分子式:C22H19ClF3N5O2
分子量:477.87
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生物活性:
CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC50 of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer.

体内研究:
CBP/p300-IN-20 (compound 28) (0.54 mg/kg; i.v.) exhibits Cmax (210 ng/mL), AUC0→∞ (102 h?ng/mL), CL (95 mL/min/kg), and T1/2 (0.3 h) in rats.

体外研究:
CBP/p300-IN-20 (compound 28) decreases Myc protein in cell-based cMyc HTRF assay, with a pEC50 of 8.5.CBP/p300-IN-20 (1 μM) shows 97% inhibition for p300 and 80% inhibition for CPB.CBP/p300-IN-20 (0.3-1000 nM; 2 h) decreases H3K18 and H3K27 acetylation without affecting H3K9 acetylation and total H3 in COLO 320HSR cells.
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