AZ505
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AZ505是通过高通量化学筛选的方法鉴定到的分子,是一种有效的和选择性的SET and MYND domain-containing 2 protein(SMYD2)抑制剂,IC50和Ki值分别为0.12 μM和0.3 μM。SMYD2是一个蛋白赖氨酸甲基转移酶,催化组蛋白(H2B、H3和H4)和非组蛋白底物(包括肿瘤抑制蛋白p53和Rb)的甲基化[1]。
AZ505是SMYD2的底物竞争性抑制剂,与多肽底物,而非辅因子竞争结合SMYD2的多肽结合沟[1]。
参考文献:
[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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 577.54 |
Cas No. | 1035227-43-0 |
Formula | C29H38Cl2N4O4 |
Solubility | Soluble in DMSO |
Chemical Name | N-cyclohexyl-3-[2-(3,4-dichlorophenyl)ethylamino]-N-[2-[2-(5-hydroxy-3-oxo-4H-1,4-benzoxazin-8-yl)ethylamino]ethyl]propanamide |
SDF | Download SDF |
Canonical SMILES | C1CCC(CC1)N(CCNCCC2=C3C(=C(C=C2)O)NC(=O)CO3)C(=O)CCNCCC4=CC(=C(C=C4)Cl)Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |