AZ505, a molecule identified from a high throughput chemical screen, is a potent and selective inhibitor of SET and MYND domain-containing 2 protein (SMYD2), a protein lysine methyltransferase catalyzing the methylation of both histone (H2B, H3 and H4) and non-histone protein substrates including the tumor suppressor proteins p53 and Rb, with the half maximal inhibition concentration IC50 and inhibition constant Ki values of 0.12 μM and 0.3 μM respectively [1].
AZ505 has been found to be a substrate competitive inhibitor of SMYD2, where it binds into the peptide binding groove of SMYD2 competing with the peptide substrates rather than the co-factor [1].
References:
[1] Ferguson AD, Larsen NA, Howard T, Pollard H, Green I, Grande C, Cheung T, Garcia-Arenas R, Cowen S, Wu J, Godin R, Chen H, Keen N. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73. doi: 10.1016/j.str.2011.06.011. Epub 2011 Jul 21.
AZ505
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| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 5mg | $177.00 | In Stock | 1 | |
| 10mg | $265.00 | Quote | -- | |
| 25mg | $370.00 | Quote | -- | |
| 50mg | $621.00 | Quote | -- | |
| 100mg | $933.00 | Quote | -- |
Citations
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Nature641, 529–536 (2025)
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Nature618, 1017–1023 (2023)
Nature610, 366–372 (2022)
Cell187(9):2288-2304 (2024)
Cell183(7):1867-1883 (2020)
Science388(6745) (2025)
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Cell Research35, 97–116 (2025)
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Description
Protocole (Protocol)
| Kinase experiment [1]: | |
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Inhibitory activities |
AZ505 binding to SMYD2 and inhibits SMYD2-mediated methylation in cells in the presence of SAM. In gastric cancer and ESCC, overexpression of SMYD2 protein was detected in 38.1% and 76.5% of patients, respectively. AZ505 inhibiting SMYD2 may be a key therapeutic strategy for these disease. |
| Cell experiment [1]: | |
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Cell |
N/A |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
N/A |
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Applications |
AZ505 inhibited SMYD2-mediated methylation in cells with IC50 value of 0.12 μM and AZ505 binding to SMYD2 is competitive with the peptide substrate and uncompetitive with the cofactor. AZ505 also inhibited other histone methyltransferases, such as SMYD3 (IC50>83.3 mM), DOT1L (IC50>83.3 mM) and EZH2 (IC50>83.3 mM) |
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References: [1] Ferguson AD, Larsen NA, Howard T, et dl. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73. | |
Documents produit (Product Documents)
Propriétés chimiques (Chemical Properties)
Utilisez les solutions mères dans les 6 mois si elles sont conservées à -80°C, ou dans le mois si elles sont conservées à -20°C.
Pour améliorer la solubilité, réchauffez le tube à 37°C et soniquez-le pendant une durée appropriée.
Calculateurs (Calculators)Molarité / Dilution / Masse moléculaire / Conversion d’unités / Formulation in vivo / Solubilité
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