Chemical Name: 2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
Biological ActivitySelective inhibitor of G9a and GLP histone lysine methyltransferases (IC50 values are < 15 nM and 19 nM for G9a and GLP respectively, and > 10000 nM for a range of other histone methyltransferases). Potently inhibits dimethylation of H3K9 in MCF-7 cells (IC50 = 70 nM). Restores metabolic and antiviral function in exhausted CD8+ T cells from patients with chronic HCV infection. Cell permeable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
Vedadi et al.
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
Liu et al.
Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection.
Barili et al.
Citation for UNC 0638
The citations listed below are publications that use Tocris products. Selected citations for UNC 0638 include:
1 Citation: Showing 1 - 1
Increased Efficacy of Histone Methyltransferase G9a Inhibitors Against MYCN-Amplified Neuroblastoma.
Authors: Bellamy Et al.
Front Oncol 2020;10
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