| Identification | Back Directory | [Name]
3-(3-(3,6-dichloro-9H-carbazol-9-yl)-2-hydroxypropyl)thiazolidine-2,4-dione | [CAS]
312631-87-1 | [Synonyms]
10074-A4
3-[3-(3,6-Dichloro-carbazol-9-yl)-2-hydroxy-propyl]-thiazolidine-2,4-dione
3-(3-(3,6-dichloro-9H-carbazol-9-yl)-2-hydroxypropyl)thiazolidine-2,4-dione
2,4-Thiazolidinedione, 3-[3-(3,6-dichloro-9H-carbazol-9-yl)-2-hydroxypropyl]- | [Molecular Formula]
C18H14Cl2N2O3S | [MDL Number]
MFCD00572945 | [MOL File]
312631-87-1.mol | [Molecular Weight]
409.29 |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [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. |
|
| Company Name: |
PHARMEKS Ltd.
|
| Tel: |
+7 (495) 702-9648 |
| Website: |
www.pharmeks.com |
|