B8063

Sigma-Aldrich

BML-210

≥98% (HPLC), powder

别名:
N1-(2-aminophenyl)-N8-phenyl-octanediamide
Empirical Formula (Hill Notation):
C20H25N3O2
CAS号:
分子量:
339.43
MDL number:
PubChem Substance ID:
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to very faintly yellow

solubility

DMSO: >20 mg/mL

storage temp.

2-8°C

SMILES string

Nc1ccccc1NC(=O)CCCCCCC(=O)Nc2ccccc2

InChI

1S/C20H25N3O2/c21-17-12-8-9-13-18(17)23-20(25)15-7-2-1-6-14-19(24)22-16-10-4-3-5-11-16/h3-5,8-13H,1-2,6-7,14-15,21H2,(H,22,24)(H,23,25)

InChI key

RFLHBLWLFUFFDZ-UHFFFAOYSA-N

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

BML-210 is a synthetic benzamide and is a potential tumor inhibitor. It is used as a therapeutic agent to treat promyelocytic leukemia. In human leukemia cell lines (NB4, HL-60, THP-1, and K562), BML-210 modulates histone deacetylase and promotes apoptosis. BML-210 favors frataxin expression in neurodegenerative disease Friedreich′s ataxia (FRDA). It interacts with myocyte enhancer factor-2 (MEF2) via hydrogen-bonding and prevents histone deacetylase 4 (HDAC4) binding.
BML-210 is a histone deacetylase inhibitor. Treatment of A549 cells with BML-210 results in a dose-dependent increase in acetylated histone levels (EC50 = 36 μM). In HeLa extracts, the IC50 for inhibition of HDAC activity is 80 μM.

Hazard Statements

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Inhibition of the function of class IIa HDACs by blocking their interaction with MEF2
Jayathilaka N, et al.
Nucleic Acids Research, 40(12), 5378-5388 (2012)
Natalia Sacilotto et al.
Genes & development, 30(20), 2297-2309 (2016-11-30)
Angiogenesis, the fundamental process by which new blood vessels form from existing ones, depends on precise spatial and temporal gene expression within specific compartments of the endothelium. However, the molecular links between proangiogenic signals and downstream gene expression remain unclear....
The novel histone deacetylase inhibitor BML-210 exerts growth inhibitory, proapoptotic and differentiation stimulating effects on the human leukemia cell lines
Savickiene J, et al.
European Journal of Pharmacology, 549(1-3), 9-18 (2006)
The histone deacetylase inhibitor BML-210 influences gene and protein expression in human promyelocytic leukemia NB4 cells via epigenetic reprogramming
Borutinskaite V and Navakauskiene R
International Journal of Molecular Sciences, 16(8), 18252-18269 (2015)
Veronika Borutinskaitė et al.
International journal of molecular sciences, 16(8), 18252-18269 (2015-08-20)
Today, cancer is understood as an epigenetic as well as genetic disease. The main epigenetic hallmarks of the cancer cell are DNA methylation and histone modifications. Proteins such as histone deacetylases (HDACs) that cause modifications of histones and other proteins...
技术文章
Epigenetic modifications are thought to occur through two key interconnected processes—DNA methylation and the covalent modification of histones.
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