AZ506 是有效的 SMYD2 抑制剂，IC50 为 17 nM。AZ506 抑制细胞中 SMYD2 甲基转移酶的活性，导致 SMYD2 介导的甲基化信号减少。
货号:ajcx37012
CAS:2043321-54-4
分子式:C33H40N6O
分子量：536.71
溶解度:DMSO : 50 mg/mL (93.16 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal[1].

AZ506 inhibits SMYD2 mediated methylation of monomethyl p53 peptide in U2OS cells with an EC50 of 1.2 μM. AZ506 inhibits SMYD2-mediated methylation (p53-me in U2OS cells) with an IC50 of 2.43 μM[1].

[1]. Cowen SD, et al. Design, Synthesis, and Biological Activity of Substrate Competitive SMYD2 Inhibitors. J Med Chem. 2016;59(24):11079-11097.