AZ505 ditrifluoroacetate
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是一种有效的SET-及MYND2-结构域蛋白2(SMYD2)抑制剂.相对于各种其它蛋白赖氨酸甲基转移酶(IC50 > 83.3 μΜ),包括SMYD3\DOT1L\EZH2\GLP\G9A和SET7/9,AZ505选择性地抑制SMYD2的酶活性(IC50: 0.12 μM)[1].
AZ505包含3个不同部分:苯并恶嗪酮基,作用于SMYD2赖氨酸结合通道;环己基,作用于SMYD2的核心SET和I-SET结构域;二氯苯基,横跨SMYD2的肽结合槽[1].
X射线晶体学分析表明,AZ505与肽底物竞争结合SMYD2的肽结合槽[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.
| Storage | Store at -20°C |
| M.Wt | 805.59 |
| Cas No. | 1035227-44-1 |
| Formula | C33H40Cl2F6N4O8 |
| Solubility | insoluble in H2O; ≥119.8 mg/mL in DMSO; ≥7.3 mg/mL in EtOH with ultrasonic |
| Chemical Name | N-cyclohexyl-3-((3,4-dichlorophenethyl)amino)-N-(2-((2-(3,5-dihydroxy-2H-benzo[b][1,4]oxazin-8-yl)ethyl)amino)ethyl)propanamide bis(2,2,2-trifluoroacetate) |
| SDF | Download SDF |
| Canonical SMILES | ClC1=C(Cl)C=C(CCNCCC(N(C2CCCCC2)CCNCCC3=C4C(N=C(O)CO4)=C(O)C=C3)=O)C=C1.FC(F)(F)C(O)=O.FC(F)(F)C(O)=O |
| 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]: | |
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抑制活性 |
在SAM 存在的细胞中，AZ505结合SMYD2并抑制SMYD2介导的甲基化。在38.1%和76.5%的胃癌和ESCC患者中检测到SMYD2蛋白的过表达。AZ505抑制SMYD2可能是这些疾病的关键治疗策略。 |
| 细胞实验 [1]: | |
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细胞系 |
N/A |
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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。 |
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反应条件 |
N/A |
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应用 |
AZ505抑制细胞中SMYD2介导的甲基化，IC50值为0.12?M。AZ505与肽底物竞争结合SMYD2，与辅因子不具有竞争性。AZ505也抑制其它组蛋白甲基转移酶，如MYD3 (IC50>83.3 mM)、DOT1L (IC50>83.3 mM)和EZH2 (IC50>83.3 mM)。 |
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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. |
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质量控制和MSDS
- 批次:
化学结构
