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UNC 0646

Cat. No. 4342

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Chemical Name: N-(1-Cyclohexyl-4-piperidinyl)-2-[hexahydro-4-(1-methylethyl)-1H-1,4-diazepin-1-yl]-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine

Biological Activity

Potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC₅₀ values are 6 nM and 15 nM for G9a and GLP, respectively). Potently blocks G9a/GLP methyltransferase activity in cells (IC₅₀ = 10 nM in MCF7 cells); exhibits low cellular toxicity (EC₅₀ = 4.7 μM in MCF7 cells). Selective for G9a/GLP over a range of other protein lysine methyltransferases and protein arginine methyltransferases.

Technical Data

M.Wt:

621.9

Formula:

C₃₆H₅₉N₇O₂

Solubility:

Soluble to 100 mM in DMSO and to 100 mM in ethanol

Purity:

>99 %

Storage:

Store at +4°C

CAS No:

1320288-17-2

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Liu et al (2011) Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J.Med.Chem. 54 6139. PMID: 21780790.

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Keywords: UNC 0646, supplier, UNC0646, epigenetics, SGC, G9a, GLP, histone, protein, lysine, methyltransferases, PKMTs, HMTs, potent, selective, inhibitors