3-(3-(3,6-dichloro-9H-carbazol-9-yl)-2-hydroxypropyl)thiazolidine-2,4-dione

10074-A4 is a c-Myc inhibitor. 10074-A4 could bind to c-Myc370-409 at different sites along the peptide chain. 10074-A4 has anticancer effects[1][2].

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> c-Myc

10074-A4 shows inhibitory activity of HL-60 cells with an IC50 of 15.1 μM[1]. 10074-A4 (25-50 μM; 24 hours) arrests the cell cycle at the S-phase in a dose-dependent manner in HL-60 cells. 10074-A4 inhibits the mRNA level of the c-Myc target genes, CCND2 and CDK4[1]. 10074-A4 could bind to c-Myc370-409 at different sites along the peptide chain and its binding behavior could be described as a ‘ligand cloud’. Even in the bound state, the structure of the c-Myc370-409 peptide remained a dynamic ensemble. The 10074-A4 ligand bound at different sites throughout the c-Myc370-409 chain with different strength[2]. Cell Viability Assay[1] Cell Line: HL-60 cells Concentration: 25 μM, 50 μM Incubation Time: 24 hours Result: Arrested the cell cycle at the S-phase.

[1]. Chen Yu, et al. Structure-based Inhibitor Design for the Intrinsically Disordered Protein c-Myc. Sci Rep. 2016 Mar 2;6:22298.

[2]. Fan Jin, et al. Ligand clouds around protein clouds: a scenario of ligand binding with intrinsically disordered proteins. PLoS Comput Biol. 2013;9(10):e1003249.