SMYD2 Inhibitor, AZ505

A cell-permeable benzooxazinyl-ethylaminoethyl-propanamide compound that acts as a potent and reversible inhibitor of SMYD2 (IC₅₀ = 120 nM, K_i = 300 nM, K_d = 500 nM). Shown to bind to the peptide-binding groove of the enzyme. This binding is dependent on the presence of S-adenosylmethionine (SAM). The inhibition appears to be competitive with respect to substrate and uncompetitive with respect to SAM. Displays ~700-fold greater selectivity over SMYD3, DOT1L, EZH2, GLP, G9a and SET7/9 protein lysine methyl transferases (IC₅₀ >83.3 µM). Inhibits SMYD2-mediated p53-K370 methylation in U2OS cells (at ~10 µM), but does not affect methylation in cells transfected with a Y240F mutant.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

AZ505 is a cell-permeable, potent, reversible inhibitor of SMYD2 (IC₅₀ = 120 nM, K_i = 300 nM) that binds to the peptide-binding groove of the enzyme.

Cell permeable: yes

Primary Target
SMYD2

Supplied as a di-trifluoroacetate salt.

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Use only fresh DMSO for reconstitution.

Ferguson, A.D., et al. 2011. Structure19, 1262.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)