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312631-87-1

312631-87-1 structure
312631-87-1 structure

Name 10074-a4
Synonyms 3-[3-(3,6-dichlorocarbazol-9-yl)-2-hydroxypropyl]thiazolidine-2,4-dione
3-[3-(3,6-dichloro-9H-carbazol-9-yl)-2-hydroxypropyl]-1,3-thiazolidine-2,4-dione
Description 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].
Related Catalog
In Vitro 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.
References

[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.

Molecular Formula C18H14Cl2N2O3S
Molecular Weight 409.28600
Exact Mass 408.01000
PSA 87.84000
LogP 4.09550