UNC 0642

Cat. No. 5132

UNC 0642 C29H44F2N6O2 [1481677-78-4]

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Chemical Name: 2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine

Biological Activity

Potent and selective G9a and GLP histone lysine methyltransferase inhibitor (IC50 < 2.5 nM). Exhibits >2,000-fold selectivity for G9a and GLP over PRC2-EZH2 and >20,000-fold selectivity over other methyltransferases. Reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50 = 110 nM). Displays modest brain penetration in vivo.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the UNC 0642 probe summary on the SGC website.

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

M.Wt:
546.7
Formula:
C29H44F2N6O2
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in 1eq. HCl
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
1481677-78-4

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 Data Sheet

Liu et al (2013) Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J.Med.Chem. 56 8931. PMID: 24102134.

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Keywords: UNC 0642, supplier, UNC0642, potent, selective, G9a, GLP, histone, lysine, methyltransferase, inhibits, inhibitors, HMTs, HMTases, epigenetics, modifications, H3K9, H3K9me2, sgc, Tocris Bioscience, Lysine Methyltransferase Inhibitor products

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