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Description: 10074-G5 is a potent inhibitor of c-Myc-Max dimerization and interaction with an IC50 of 146 uM and with anticancer activities. 10074-G5 binds to and distorts the bHLH-ZIP domain of c-Myc, thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity. In vitro, 10074-G5 inhibited the growth of Daudi Burkitt's lymphoma cells and disrupted c-Myc/Max dimerization. 10074-G5 had no effect on the growth of Daudi xenografts in C.B-17 SCID mice that were treated with 20 mg/kg 10074-G5 intravenously for 5 consecutive days. Inhibition of c-Myc/Max dimerization in Daudi xenografts was not seen 2 or 24 h after treatment.
References: Bioorg Med Chem Lett. 2013 Jan 1; 23(1):370-4; J Pharmacol Exp Ther. 2010 Dec; 335(3):715-27.
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