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AZ505 ditrifluoroacetate

CAS No. : 1035227-44-1

產(chǎn)品活性：AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC₅₀ of 0.12 μM.

研究領(lǐng)域：Epigenetics

作用靶點(diǎn)：Histone Methyltransferase

In Vitro: 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 K_d of 0.5 μM. In contrast, the calculated K_d 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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