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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-AZ506
AZ506

Chemical Structure : AZ506

CAS No.: 2043321-54-4

AZ506 (SMYD2 inhibitor AZ506, AZ-506)

货号: PC-22290Not For Human Use, Lab Use Only.

AZ506 is a potent, selective inhibitor of protein lysine methyltransferase SMYD2 with IC50 of 17 nM, inhibits SMYD2 mediated methylation of monomethyl p53 peptide in U2OS cells with IC50 of 1.02 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AZ506 is a potent, selective inhibitor of protein lysine methyltransferase SMYD2 with IC50 of 17 nM, inhibits SMYD2 mediated methylation of monomethyl p53 peptide in U2OS cells with IC50 of 1.02 uM.
AZ506 is selective for SMYD2 but do possess limited activity against DOT1L, in a focused panel of KMTs including EZH2, NSD1, G9a SMYD2, and DOT1L.
AZ506 works in a p53-dependent manner to affect cell proliferation in a panel of matched paired p53 wild-type and p53-null colorectal cancer cell lines.

物理化学性质&存储条件

分子量 536.72
分子式 C33H40N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(2-(4-(2-(1H-Indol-3-yl)ethyl)piperazin-1-yl)phenyl)-N-(3-(pyrrolidin-1-yl)propyl)nicotinamide

参考文献

1. Scott D. Cowen, et al. J. Med. Chem. 2016, 59, 24, 11079–11097.

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