| Identification | Back Directory | [Name]
AZ-505 | [CAS]
1035227-44-1 | [Synonyms]
AZ-505
AZ-505;AZ505;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) | [Molecular Formula]
C33H40Cl2F6N4O8 | [MOL File]
1035227-44-1.mol | [Molecular Weight]
805.589 |
| Hazard Information | Back Directory | [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]. |
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SPIRO PHARMA
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BOC Sciences
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Musechem
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DC Chemicals
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