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AZ506

Chemical Structure : AZ506

CAS No.: 2043321-54-4

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
Shipping
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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