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编 号:F762977
分子式:C44H50N4O11S2
分子量:875.02
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生物活性:
NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc.

体内研究:
NC-III-49-1 shows metabolic stability in human and mouse liver microsomes with an T1/2 values of <2.3, <2.3 min, respectively.

体外研究:
NC-III-49-1 (0-10 μM; 72 h) shows antiproliferative activity with an IC50 value of 0.69 nM in MM1.S cells.NC-III-49-1 (0-10 μM; 6 h) decreases the expression of c-Myc in a dose dependent manner..NC-III-49-1 shows inhibition by interact with both KAc sites.
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