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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-AZ505
AZ505

Chemical Structure : AZ505

CAS No.: 1035227-43-0

AZ505 (AZ-505;AZ 505)

货号: PC-44245Not For Human Use, Lab Use Only.

AZ505 (AZ-505, AZ 505) is a potent and selective inhibitor of protein lysine methyltransferase SMYD2 with IC50 of 0.12 uM, displays >600-fold against other histone methyltransferases, such as SMYD3 and EZH2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZ505 (AZ-505, AZ 505) is a potent and selective inhibitor of protein lysine methyltransferase SMYD2 with IC50 of 0.12 uM, displays >600-fold against other histone methyltransferases, such as SMYD3 and EZH2.
AZ505 suppresses BMP2-induced SMAD1/5 phosphorylation, delays cyst growth in both early- and later-stage Pkd1 conditional knockout mouse models.
AZ505 also significantly reduced tumor growth in vivo in triple-negative breast cancer (TNBC) models.

物理化学性质&存储条件

分子量 577.5424
分子式 C29H38Cl2N4O4
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

Propanamide, N-cyclohexyl-3-[[2-(3,4-dichlorophenyl)ethyl]amino]-N-[2-[[2-(3,4-dihydro-5-hydroxy-3-oxo-2H-1,4-benzoxazin-8-yl)ethyl]amino]ethyl]-

参考文献

1. Ferguson AD, et al. Structure. 2011 Sep 7;19(9):1262-73.

2. Gao S, et al. J Biol Chem. 2017 Jul 28;292(30):12702-12712.

3. Li LX, et al. J Clin Invest. 2017 Jun 30;127(7):2751-2764.

4. Li LX, et al. Cell Death Dis. 2018 Feb 27;9(3):326.

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