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標(biāo)簽:BML-210(CAY10433)
聯(lián)系人:高小姐
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化學(xué)性質(zhì):
規(guī)格 | 10mM (in 1mL DMSO) 5mg 10mg 50mg |
CAS | 537034-17-6 |
別名 |
|
化學(xué)名 | (1Z,8Z)-N'1-(2-aminophenyl)-N'8-phenyloctanebis(imidic acid) |
分子式 | C20H25N3O2 |
分子量 | 339.43 |
溶解度 | ≥ 10.5mg/mL in DMSO |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述:
Histone deacetylases (HDACs) are a class of enzymes that remove acetyl groups from ε-N-acetyl lysines on histones, allowing the histones to wrap the DNA more tightly. DNA expression is regulated by de-acetylation and acetylation.
BML-210 (CAY10433) is a novel HDAC inhibitor. In FRDA lymphoid cell line (GM15850), BML-210 increased the level of FXN mRNA by 1.4-fold [1]. In the human leukemia cell lines (NB4, HL-60, THP-1, and K562), BML-210 induced G1 arrest and histone H4 acetylation, affected NF-κB and Sp1 binding to the p21 or the FasL promoters, and influenced expression of Sp1, NF-κB, p21 and FasL. BML-210 inhibited cell growth and induced apoptosis in a time- and dose-dependent way. BML-210 also induced K562 and HL-60 cell differentiation (up to 30%) to erythrocytes and granulocytes, respectively [2]. In HeLa cells, BML-210 (20 or 30 μM) increased the amount of cells in G0/G1 phase, caused sub-G1 accumulation, and induced apoptosis [3]. In human promyelocytic leukemia NB4 cells, BML-210 inhibited cell growth in a dose- and time-dependent way [4].
References:
[1]. Herman D, Jenssen K, Burnett R, et al. Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. Nat Chem Biol, 2006, 2(10): 551-558.
[2]. Savickiene J, Borutinskaite VV, Treigyte G, et al. The novel histone deacetylase inhibitor BML-210 exerts growth inhibitory, proapoptotic and differentiation stimulating effects on the human leukemia cell lines. Eur J Pharmacol, 2006, 549(1-3): 9-18.
[3]. Borutinskaite VV, Magnusson KE, Navakauskiene R. Histone deacetylase inhibitor BML-210 induces growth inhibition and apoptosis and regulates HDAC and DAPC complex expression levels in cervical cancer cells. Mol Biol Rep, 2012, 39(12): 10179-10186.
[4]. Borutinskait? V, Navakauskien? R. The Histone Deacetylase Inhibitor BML-210 Influences Gene and Protein Expression in Human Promyelocytic Leukemia NB4 Cells via Epigenetic Reprogramming. Int J Mol Sci, 2015, 16(8): 18252-18269.
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