货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S81781-5mg	≥99%	￥820.00 S81781-5mg ￥820.00 3-5天	0 货期：3-5天	-	-	-	-
S81781-10mg	≥99%	￥1630.00 S81781-10mg ￥1630.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S81781-5mg

≥99%

￥820.00

货期：3-5天

S81781-10mg

≥99%

￥1630.00

货期：3-5天

产品描述：

AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.

靶点：

IC50: 0.12 μM (SMYD2);HistoneMethyltransferase

体外研究：

AZ505 ditrifluoroacetate is highly selective and shows an activity at submicromolar concentrations in vitro. The IC50 of AZ505 ditrifluoroacetate for SMYD2 is 0.12 μM, which is >600-fold greater than the IC50s of AZ505 ditrifluoroacetate for other histone methyltransferases, such as SMYD3 (IC50>83.3 μM), DOT1L (IC50>83.3 μM) and AZ505 ditrifluoroacetate (IC50>83.3 μM). AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with an IC50 of 0.12 μM. The human SMYD (SET and MYND domain-containing protein) family of protein lysine methyltransferases contains five members (SMYD1-5). Moreover, AZ505 ditrifluoroacetate fails to inhibit the enzymatic activities of a panel of protein lysine methyltransferases. AZ505 ditrifluoroacetate is nominated for ITC binding study with Kd of 0.5 μM. In contrast, the calculated Kd for the p53 substrate peptide is 3.7 μM. AZ505 ditrifluoroacetate binding to SMYD2 is driven primarily by entropy, which often suggests that binding is mediated by hydrophobic interactions with few specific hydrogen bonds

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.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.241 ml	6.207 ml	12.413 ml
5 mM	0.248 ml	1.241 ml	2.483 ml
10 mM	0.124 ml	0.621 ml	1.241 ml
50 mM	0.025 ml	0.124 ml	0.248 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

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计算重置

AZ505 (ditrifluoroacetate)