貨號	規格	價格	上海	北京	武漢	南京	購買數量
S81781-5mg	≥99%	￥2250.00 S81781-5mg ￥2250.00 2-3天	0 貨期：2-3天	-	-	-
S81781-10mg	≥99%	￥4450.00 S81781-10mg ￥4450.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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

產品描述：

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

靶點：

IC50: 0.12 μM (SMYD2);HistoneMethyltransferase

體外研究：

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

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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AZ505 (ditrifluoroacetate)