10074-A4 

10074-A4 is a c-Myc inhibitor. 10074-A4 could bind to c-Myc_370-409 at different sites along the peptide chain. 10074-A4 has anticancer effects^[1][2].

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-Myc_370-409 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-Myc_370-409 peptide remained a dynamic ensemble. The 10074-A4 ligand bound at different sites throughout the c-Myc_370-409 chain with different strength^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

409.29

Solid

C₁₈H₁₄Cl₂N₂O₃S

312631-87-1

O=C(SCC1=O)N1CC(CN2C3=C(C=C(C=C3)Cl)C4=C2C=CC(Cl)=C4)O

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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

  [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.  [Content Brief]