UNC 0642
Chemical Name: 2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
Purity: ≥99%
Biological Activity
UNC 0642 is a potent and selective G9a and GLP histone lysine methyltransferase inhibitor (IC50 < 2.5 nM) that exhibits >2,000-fold selectivity for G9a and GLP over PRC2-EZH2 and >20,000-fold selectivity over other methyltransferases. UNC 0642 reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50 = 110 nM), and displays modest brain penetration in vivo.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 UNC0642 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 biology toolbox to study protein methyltransferases and epigenetic signaling.
Scheer et al.
Nat.Commun., 2019;10:19 -
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
Liu et al.
J.Med.Chem., 2013;56:8931
Product Datasheets
Citations for UNC 0642
The citations listed below are publications that use Tocris products. Selected citations for UNC 0642 include:
3 Citations: Showing 1 - 3
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EHMT2 methyltransferase governs cell identity in the lung and is required for KRAS G12D tumor development and propagation.
Authors: Xi Et al.
Elife 2022;11
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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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Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis.
Authors: Xin Et al.
Cell 2019;176:1113-1127.e16
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