10074-G5

10074-G5 (413611-93-5) inhibits c-Myc by disrupting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity.1 10074-G5 binds to the c-Myc bHLHZip domain with Kd=2.8 mM.1 It was cytotoxic in C-Myc-overexpressing cell lines (IC50s = 13 to 15 mM) but was not active in vivo due to rapid metabolism.2 10074-G5 is a useful tool to probe for involvement of c-Myc involvement in cellular processes.3,4 Binds to and sequesters the intrinsically disordered amyloid-β (Aβ) in its monomeric soluble state and rescues a C. elegans model of Aβ-associated toxicity.5 References/Citations: Follis et al. (2008), Structural rationale for the coupled binding and unfolding of the c-Myc oncoprotein by small molecules; Chem..Biol. 15 1149 Clausen et al. (2010), In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization; J. Pharmacol. Exp. Ther. 335 715 Velpula et al. (2012), Transcriptional repression