UNC 0638
Chemical Name: 2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
Purity: ≥98%
Biological Activity
UNC 0638 is a selective 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.External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of UNC 0638 is reviewed on the chemical probes website.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
Vedadi et al.
Nat.Chem.Biol., 2011;7:566 -
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
Liu et al.
J.Med.Chem., 2011;54:6139 -
Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection.
Barili et al.
Nat.Commun., 2020;11:604
Product Datasheets
Citations for UNC 0638
The citations listed below are publications that use Tocris products. Selected citations for UNC 0638 include:
4 Citations: Showing 1 - 4
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G9a Promotes Breast Cancer Recurrence through Repression of a Pro-inflammatory Program.
Authors: Jen-Tsan Et al.
Cell Rep 2020;33:108341
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Increased Efficacy of Histone Methyltransferase G9a Inhibitors Against MYCN-Amplified Neuroblastoma.
Authors: Bellamy Et al.
Front Oncol 2020;10
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Suppression of STING Associated with LKB1 Loss in KRAS-Driven Lung Cancer.
Authors: Elena Et al.
Cancer Discov 2019;9:34-45
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Loss of G9a preserves mutation patterns but increases chromatin accessibility, genomic instability and aggressiveness in skin tumours.
Authors: Mercè Et al.
Nat Cell Biol 2018;20:1400-1409
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