10074-A4 是一种 c-Myc 抑制剂，可以在肽链的不同位点与 c-Myc370-409 结合。10074-A4 具有抗癌作用。
货号:ajcx35952
CAS:312631-87-1
分子式:C18H14Cl2N2O3S
分子量：409.29
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

[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.