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AM114

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Chemical Structure| 856849-35-9 同义名 : PS-IX;Proteasome inhibitor IX
CAS号 : 856849-35-9
货号 : A817591
分子式 : C20H21B2NO5
纯度 : 98%+
分子量 : 377.007
MDL号 : MFCD09971093
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(13.26 mM)，配合低频超声助溶，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 AM114 is a chalcone derivative that inhibits chymotrypsin-like activity of the 20S proteasome with an IC50 value of about 1 μM. AM114 has the activity of inhibiting the growth of HCT116 p53+/+ cells with an IC50 value of 1.49 μM. AM114 has strong anticancer activity[1][2].Due to the inhibition of chymotrypsin-like activity of the 20S proteasome in vitro, AM114 leads to a massive accumulation of ubiquitinated p53 and other cellular proteins throughout the cell. At a concentration of 1µM for 14 days, AM114 reduced the viability of p53+/+ and p53-/- cells by approximately 70% and 20%, respectively. In contrast, AM114 caused apoptosis in 28% of HCT116 p53+/+ cells after 48 hours of action, and the proportion of apoptotic cells increased to 76% after 72 hours of treatment. In a colony formation assay, AM114 showed potent activity against p53+/+ cells carrying p53+/+ with an IC50 value of 0.6 µM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.65mL

0.53mL

0.27mL

13.26mL

2.65mL

1.33mL

26.52mL

5.30mL

2.65mL
参考文献

[1]Geetha Achanta , et al. A Boronic-Chalcone Derivative Exhibits Potent Anticancer Activity Through Inhibition of the Proteasome. Mol Pharmacol. 2006 Jul;70(1):426-33.

[2]Encouse B Golden, et al. Green Tea Polyphenols Block the Anticancer Effects of Bortezomib and Other Boronic Acid-Based Proteasome Inhibitors. Blood. 2009 Jun 4;113(23):5927-37.