化学性质:
规格 | 5mg 10mg 25mg 50mg 100mg |
CAS | 1035227-44-1 |
别名 |
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化学名 | N-cyclohexyl-3-((3,4-dichlorophenethyl)amino)-N-(2-((2-(3,5-dihydroxy-2H-benzo[b][1,4]oxazin-8-yl)ethyl)amino)ethyl)propanamide bis(2,2,2-trifluoroacetate) |
分子式 | C33H40Cl2F6N4O8 |
分子量 | 805.59 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
AZ505 is a potent SET and MYND domain-containing 2 protein (SMYD2) inhibitor that selectively inhibits the enzymatic activity of SMYD2 (IC50: 0.12 μM) over a variety of other protein lysine methyltransferases (IC50 > 83.3 μΜ), including SMYD3, DOT1L, EZH2, GLP, G9A and SET7/9 [1].
AZ505 contains three distinct moieties: the benzooxazinone group which interacts with the lysine-binding channel of SMYD2; the cyclohexyl group which interacts with the core SET and I-SET domains of SMYD2; and the dichlorophenethyl group which extends across the peptide binding groove of SMYD2 [1].
The X-ray crystallographic analysis has revealed that AZ505 binds into the peptide binding groove of SMYD2 competing with the peptide substrates [1].
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