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Daminozide

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产品名称: Daminozide
产品型号: GOY-Y3562
产品展商: 谷研
产品文档: 无相关文档
发布时间:2023-05-08

简单介绍

DaminozideDMF: 5 mg/ml,DMSO: 11 mg/ml,PBS (pH 7.2): 2 mg/ml


Daminozide  的详细介绍


性能参数

产品名称

Daminozide

规格

10mM (in 1mL DMSO) 25g 50g

货号

GOY-Y3562

 含量

>98.00%

CAS

1596-84-5

别名

Alar;B 995;DMASA;SADH;Succinic Acid; Aminozide;Kylar;DIMG

 

 

化学名

4-(2,2-dimethylhydrazinyl)-4-oxobutanoic acid

分子式

C6H12N2O3

分子量

分子量 160.17

溶解度

DMF: 5 mg/ml,DMSO: 11 mg/ml,PBS (pH 7.2): 2 mg/ml

储存条件

Store at -20°C

General tips

 

用途

仅供科研

价格

电询

详细内容

Daminozide, a plant growth regulator, selectively inhibits the KDM2A with IC50 value of 1.5 μM, PHF8 with IC50 value of 0.55 μM, KDM7A with IC50 value of 2 μM.[1]

FBXL11/KDM2A is a histone H3 lysine 36 demethylase enzyme which enzymatic activity relies on a conserved JmjC domain in the N-terminus of the protein that coordinates iron and alphaketoglutarate to catalyze demethylation via a hydroxylation based mechanism.[2] The ZF-CxxC DNA binding domain within FBXL11/KDM2A has the capacity to interact with non-methylated DNA and can target to CpG island regions of the genome where it specifically removes histone H3 lysine 36 methylation.[3] This mechanism acts to create a chromatin environment at CpG islands that highlights these regulatory elements and differentiates them from non-regulatory regions in large complex mammalian genomes. In a study in mouse hepatocytes, this gene was shown to regulate hepatic gluconeogenesis.[4]

Histone Nε-methyl lysine demethylases KDM2/7 have been identified as potential targets for cancer therapies. Lung cancer is the leading cause of cancer deaths in the United States and worldwide. Non–small cell lung cancer (NSCLC)accounts for about 85% of all lung cancer cases, and its molecular etiology is heterogeneous[5]. Klaus W. et al [6] found that KDM2A overexpression in NSCLC cells increased cell proliferation and invasiveness.And KDM2A knockdown abrogated tumor growth and invasive abilities of NSCLC cells in mouse xenograft models, suggesting that KDM2A may be a promising therapeutic target in NSCLC.Daminozide, as a KDM2A selective inhibitor, was once widely used as a plant growth retardant but now will be a potent approach to targeted therapies for NSCLC.[7]

 

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