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The Novel Histone Deacetylase Inhibitor BML-210 Exerts Growth Inhibitory, Proapoptotic and Differentiation Stimulating Effects on the Human Leukemia Cell Lines

The Novel Histone Deacetylase Inhibitor BML-210 Exerts Growth Inhibitory, Proapoptotic and Differentiation Stimulating Effects on the Human Leukemia Cell Lines

Jurate Savickiene, Veronika-Viktorija Borutinskaite, Grazina Treigyte, Karl-Eric Magnusson, Ruta Navakauskiene

Eur J Pharmacol. 2006 Nov 7;549(1-3):9-18.

PMID: 16978604

Abstract:

Histone deacetylase inhibitors have a potent role in the strategy for the treatment of leukemias. BML-210 (N-(2-Aminophenyl)-N' phenyloctanol diamine) is the novel histone deacetylase inhibitor, and its mechanism of action has not been characterized. In this study, we examined the in vitro effects of BML-210 on the human leukemia cell lines (NB4, HL-60, THP-1, and K562). We found that BML-210 inhibits the growth of all cell lines and promotes apoptosis in a dose- and time-dependent manner. BML-210 alone induces HL-60 and K562 cell differentiation (up to 30%) to granulocytes and erythrocytes, respectively, and in combination with differentiation agents - all-trans retinoic acid and hemin, markedly potentates it. Those treatments cause G1 arrest and histone H4 acetylation, affects transcription factor NF-kappaB and Sp1 binding activity to their consensus sequences, the p21 or the FasL promoters, and influences expression of Sp1, NF-kappaB, p21 and FasL. These findings suggest that BML-210 could be a promising antileukemic agent to induce apoptosis and to modulate differentiation through the modulation of histone acetylation and gene expression.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP537034176	BML-210		537034-17-6	Price

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