产品
编 号：F015468
分子式：C33H40Cl2F6N4O8
分子量：805.59
分子式：C33H40Cl2F6N4O8
分子量：805.59
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1035227-44-1
产品详情
生物活性：
AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
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.
AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
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.
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