AZ505 ditrifluoroacetate

AZ505 二三氟乙酸盐

AZ505 ditrifluoroacetate

A656142-1ml

1ml

10mM in DMSO

干燥,-80℃储存

超低温冰袋运输

AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC 50 of 0.12 μM. In Vitro AZ505 ditrifluoroacetate is highly selective and shows an activity at submicromolar concentrations in vitro. The IC 50 of AZ505 ditrifluoroacetate for SMYD2 is 0.12 μM, which is >600-fold greater than the IC 50 s of AZ505 ditrifluoroacetate for other histone methyltransferases, such as SMYD3 (IC 50 >83.3 μM), DOT1L (IC 50 >83.3 μM) and AZ505 ditrifluoroacetate (IC 50 >83.3 μM). AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with an IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IC50: 0.12 μM (SMYD2)

AZ505 二三氟乙酸酯是一种强效的选择性 SMYD2 抑制剂，其 IC 50 为 0.12 μM。

1035227-44-1(DMSO)

C33H40Cl2F6N4O8

805.6 g/mol

C1CCC(CC1)N(CCNCCC2=C3C(=C(C=C2)O)NC(=O)CO3)C(=O)CCNCCC4=CC(=C(C=C4)Cl)Cl.C(=O)(C(F)(F)F)O.C(=O)(C(F)(F)F)O