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BML-210(CAY10433)

Catalog No.
B5968
HDAC抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 880.00
现货
5mg
¥ 800.00
现货
10mg
¥ 1,200.00
现货
50mg
¥ 5,000.00
现货

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Background

BML-210(CAY10433)是一种新型的HDAC抑制剂,其IC50值为87 μM[1].

组蛋白去乙酰化酶(HDACs)从组蛋白的ε-N-乙酰赖氨酸上移除乙酰基,使组蛋白更紧密地包裹DNA.DNA表达由去乙酰化和乙酰化调节.

BML-210(CAY10433)是一种新型的HDAC抑制剂.在FRDA淋巴细胞系(GM15850)中,BML-210使FXN mRNA水平增加1.4倍[1].在人白血病细胞系(NB4\HL-60\THP-1和K562)中,BML-210诱导G1期阻滞以及组蛋白H4乙酰化,影响NF-κB和Sp1结合p21启动子或FasL启动子,并影响Sp1\NF-κB\p21以及FasL表达.BML-210时间与剂量依赖性地抑制细胞生长并诱导细胞凋亡.BML-210也诱导K562和HL-60细胞(高达30%)分别分化为红细胞和粒细胞[2].在HeLa细胞中,BML-210(20 μM或30 μM)增加G0/G1期细胞数量,引起亚G1期累积,并诱导细胞凋亡[3].在人早幼粒白血病NB4细胞中,BML-210剂量与时间依赖性地抑制细胞生长[4].

参考文献:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt339.43
Cas No.537034-17-6
FormulaC20H25N3O2
Solubility≥10.5mg/mL in DMSO
Chemical Name(1Z,8Z)-N'1-(2-aminophenyl)-N'8-phenyloctanebis(imidic acid)
SDFDownload SDF
Canonical SMILESNC1=CC=CC=C1/[*]=C(O)/CCCCCC/C(O)=N/C2=CC=CC=C2
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

化学结构

BML-210(CAY10433)