UNC 0646

Cat. No. 4342

UNC 0646 C36H59N7O2 [1320288-17-2]

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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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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, inhibits, Tocris Bioscience, Lysine Methyltransferase Inhibitor products

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