切换导航

AZ505

现货
Catalog No.
B1255
SMYD2抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 2,940.00
Please inquiry
10mg
¥ 5,340.00
Please inquiry
25mg
¥ 8,160.00
Please inquiry
50mg
¥ 13,440.00
Please inquiry
100mg
¥ 20,750.00
Please inquiry

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

AZ505, a molecule identified from a high throughput chemical screen, is a potent and selective inhibitor of SET and MYND domain-containing 2 protein (SMYD2), a protein lysine methyltransferase catalyzing the methylation of both histone (H2B, H3 and H4) and non-histone protein substrates including the tumor suppressor proteins p53 and Rb, with the half maximal inhibition concentration IC50 and inhibition constant Ki values of 0.12 μM and 0.3 μM respectively [1].
AZ505 has been found to be a substrate competitive inhibitor of SMYD2, where it binds into the peptide binding groove of SMYD2 competing with the peptide substrates rather than the co-factor [1].
References:
[1] Ferguson AD, Larsen NA, Howard T, Pollard H, Green I, Grande C, Cheung T, Garcia-Arenas R, Cowen S, Wu J, Godin R, Chen H, Keen N. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73. doi: 10.1016/j.str.2011.06.011. Epub 2011 Jul 21.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt577.54
Cas No.1035227-43-0
FormulaC29H38Cl2N4O4
SolubilitySoluble in DMSO
Chemical NameN-cyclohexyl-3-[2-(3,4-dichlorophenyl)ethylamino]-N-[2-[2-(5-hydroxy-3-oxo-4H-1,4-benzoxazin-8-yl)ethylamino]ethyl]propanamide
SDFDownload SDF
Canonical SMILESC1CCC(CC1)N(CCNCCC2=C3C(=C(C=C2)O)NC(=O)CO3)C(=O)CCNCCC4=CC(=C(C=C4)Cl)Cl
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。

试验操作

激酶实验[1]:

抑制活性

在细胞中存在SAM的条件下,AZ505与SMYD2结合,从而抑制SMYD2介导的甲基化。在胃癌和ESCC中,分别在38.1%和76.5%的患者中检测到SMYD2蛋白过表达。AZ505抑制SMYD2可能是治疗这些疾病的关键策略。

细胞实验: [1]

细胞系

N/A

制备方法

溶于DMSO,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

N/A

实验结果

AZ505抑制细胞中SMYD2介导的甲基化,IC50值为0.12 μM,AZ505与肽底物竞争结合SMYD2,与辅因子无竞争性。AZ505还抑制其它组蛋白甲基转移酶,例如SMYD3、DOT1L和EZH2,IC50均大于83.3 mM

References:

[1] Ferguson AD, Larsen NA, Howard T, et dl. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73.

质量控制

质量控制和MSDS

批次:

化学结构

AZ505