UNC 0642

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Cat.No. 5132 - UNC 0642 | C29H44F2N6O2 | CAS No. 1481677-78-4
Description: Potent and selective G9a and GLP inhibitor
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% (HPLC)
Datasheet
Citations
Reviews
Literature

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.

Compound Libraries

UNC 0642 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 546.7
Formula C29H44F2N6O2
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1481677-78-4
PubChem ID 53315878
InChI Key RNAMYOYQYRYFQY-UHFFFAOYSA-N
Smiles CC(C)N(CC4)CCC4NC1=C2C(C=C(OCCCN3CCCC3)C(OC)=C2)=NC(N5CCC(F)(F)CC5)=N1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 54.67 100
1eq. HCl 27.34 50

Preparing Stock Solutions

The following data is based on the product molecular weight 546.7. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.83 mL 9.15 mL 18.29 mL
5 mM 0.37 mL 1.83 mL 3.66 mL
10 mM 0.18 mL 0.91 mL 1.83 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

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References

References are publications that support the biological activity of the product.

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


If you know of a relevant reference for UNC 0642, please let us know.

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View all G9a/GLP Inhibitors

Keywords: UNC 0642, UNC 0642 supplier, UNC0642, potent, selective, G9a, GLP, histone, lysine, methyltransferase, inhibits, inhibitors, HMTs, HMTases, epigenetics, modifications, H3K9, H3K9me2, sgc, Lysine, Methyltransferases, G9a/GLP, 5132, Tocris Bioscience

Citations for UNC 0642

Citations are publications that use Tocris products.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.