AZ505

AZ505

Catalog Number:
L002369887APE
Mfr. No.:
APE-B1255
Price:
$426
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Alternative Name
          N-cyclohexyl-3-[2-(3,4-dichlorophenyl)ethylamino]-N-[2-[2-(5-hydroxy-3-oxo-4H-1,4-benzoxazin-8-yl)ethylamino]ethyl]propanamide
          CAS Number
          1035227-43-0
          Molecular Formula
          C29H38Cl2N4O4
          Molecular Weight
          577.54
          Appearance
          A crystalline solid
          Purity
          98.00%
          Solubility
          Soluble in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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