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| Product Name: | AZ-505 | | Synonyms: | AZ-505;AZ505 (ditrifluoroacetate);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]propanamide 2,2,2-trifluoroacetate (1:2);AZ-505 2TFA salt;AZ-505;AZ505;AZ 505;N-cyclohexyl-3-((3,4-dichlorophenethyl)amino)-N-(2-((2-(5-hydroxy-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)ethyl)amino)ethyl)propanamide bis(2,2,2-trifluoroacetate) | | CAS: | 1035227-44-1 | | MF: | C31H39Cl2F3N4O6 | | MW: | 691.57 | | EINECS: | | | Product Categories: | | | Mol File: | 1035227-44-1.mol |  |
| | AZ-505 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | insoluble in H2O; ≥119.8 mg/mL in DMSO; ≥7.3 mg/mL in EtOH with ultrasonic | | form | Powder | | color | White to light yellow |
| | AZ-505 Usage And Synthesis |
| Uses | AZ505 is a potent inhibitor of SMYD2, which plays an important role in epigenetic signalling. Inhibiition of SMYD2 also functions as an activator of the tumor suppressor proteins. | | Biological Activity | 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]. |
| | AZ-505 Preparation Products And Raw materials |
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