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Description: AZ505 ditrifluoroacetate is a novel, potent and highly selective inhibitor of SMYD2 with an IC50 of 0.12 uM and with potential anticancer activity. AZ505 is composed of three benzooxazinone, cyclohexyl, and dichlorophenethyl substituents. The structure of the ternary complex reveals that a single AZ505 molecule is bound in the peptide binding groove of SMYD2.
References:
1. Komatsu S, et al. Overexpression of SMYD2 contributes to malignant outcome in gastric cancer. Br J Cancer. 2015 Jan 20; 112(2):357-64.
2. Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7; 19(9):1262-73.
3. Li LX, et al. Lysine methyltransferase SMYD2 promotes cyst growth in autosomal dominant polycystic kidney disease. J Clin Invest. 2017 Jun 30; 127(7):2751-2764.
Related CAS #: 1035227-43-0 (free base) 1035227-44-1 (TFA)
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