AZ506 | SMYD2 inhibitor | Probechem Biochemicals

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Chemical Structure : AZ506

AZ506 (SMYD2 inhibitor AZ506, AZ-506)

Catalog No.: PC-22290Not For Human Use, Lab Use Only.

AZ506 is a potent, selective inhibitor of protein lysine methyltransferase SMYD2 with IC50 of 17 nM, inhibits SMYD2 mediated methylation of monomethyl p53 peptide in U2OS cells with IC50 of 1.02 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AZ506 is a potent, selective inhibitor of protein lysine methyltransferase SMYD2 with IC50 of 17 nM, inhibits SMYD2 mediated methylation of monomethyl p53 peptide in U2OS cells with IC50 of 1.02 uM.
AZ506 is selective for SMYD2 but do possess limited activity against DOT1L, in a focused panel of KMTs including EZH2, NSD1, G9a SMYD2, and DOT1L.
AZ506 works in a p53-dependent manner to affect cell proliferation in a panel of matched paired p53 wild-type and p53-null colorectal cancer cell lines.

Physicochemical Properties

M.Wt	536.72
Formula	C33H40N6O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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Solubility	10 mM in DMSO
Chemical Name/SMILES	5-(2-(4-(2-(1H-Indol-3-yl)ethyl)piperazin-1-yl)phenyl)-N-(3-(pyrrolidin-1-yl)propyl)nicotinamide

References

1. Scott D. Cowen, et al. J. Med. Chem. 2016, 59, 24, 11079–11097.

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AZ506 (SMYD2 inhibitor AZ506, AZ-506)

Biological Activity

Physicochemical Properties

References

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