AZ505 ditrifluoroacetate

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Chemical Structure| 1035227-44-1 同义名 : -
CAS号 : 1035227-44-1
货号 : A391113
分子式 : C33H40Cl2F6N4O8
纯度 : 99%+
分子量 : 805.589
MDL号 : MFCD28137733
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(148.96 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 ditrifluoroacetate demonstrates high selectivity and activity at submicromolar concentrations in vitro. The IC50 of AZ505 ditrifluoroacetate against SMYD2 is 0.12 μM, which is >600-fold higher than its IC50 values against other histone methyltransferases, including SMYD3 (IC50>83.3 μM), DOT1L (IC50>83.3 μM), and EZH2 (IC50>83.3 μM) [1]. AZ505 ditrifluoroacetate 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 encompasses five members (SMYD1-5). Furthermore, AZ505 ditrifluoroacetate does not inhibit the enzymatic activities of a panel of protein lysine methyltransferases. It is slated for an isothermal titration calorimetry (ITC) binding study, with a Kd of 0.5 μM. In contrast, the calculated Kd for the p53 substrate peptide is 3.7 μM. The binding of AZ505 ditrifluoroacetate to SMYD2 is primarily driven by entropy, indicative of hydrophobic interactions with limited specific hydrogen bonding [2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.24mL

0.25mL

0.12mL

6.21mL

1.24mL

0.62mL

12.41mL

2.48mL

1.24mL
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.