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AZ505

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Chemical Structure| 1035227-43-0 同义名 : -
CAS号 : 1035227-43-0
货号 : A550753
分子式 : C29H38Cl2N4O4
纯度 : 99%+
分子量 : 577.542
MDL号 : N/A
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(432.87 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 AZ505 is highly selective and shows an activity at submicromolar concentrations in vitro. The IC50 value of AZ505 against SMYD2 is 0.12 μM, representing a >600-fold difference compared to its IC50 values against other histone methyltransferases, such as SMYD3 (IC50>83.3 μM), DOT1L (IC50>83.3 μM), and EZH2 (IC50>83.3 μM) [1]. AZ505 functions as a potent and selective inhibitor of SMYD2, with an IC50 of 0.12 μM. The human SMYD (SET and MYND domain-containing protein) family comprises five members (SMYD1-5). Additionally, AZ505 does not inhibit the enzymatic activities of a range of protein lysine methyltransferases. AZ505 has been proposed for an isothermal titration calorimetry (ITC) binding study, with a Kd value of 0.5 μM. Conversely, the calculated Kd for the p53 substrate peptide is 3.7 μM. The interaction between AZ505 and SMYD2 is primarily governed by entropy, implying that binding is predominantly facilitated by hydrophobic interactions with minimal specific hydrogen bonding [2].
作用机制 AZ505 is a substrate competitive inhibitor which can bound in the peptide binding groove of SMYD2.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.66mL

1.73mL

0.87mL

17.31mL

3.46mL

1.73mL
参考文献

[1]Komatsu S, et al. Overexpression of SMYD2 contributes to malignant outcome in gastric cancer. Br J Cancer. 2015 Jan 20;112(2):357-64.

[2]Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73.