UNC 0642

Pricing Availability Delivery Time Qty
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
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
1eq. HCl 27.34 50
DMSO 54.67 100

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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 Lysine Methyltransferase Inhibitors

Keywords: UNC0642 potent selective G9a GLP histone lysine methyltransferase inhibits inhibitors HMTs HMTases epigenetics modifications H3K9 H3K9me2 sgc Lysine Methyltransferases

Citations for UNC 0642

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Literature in this Area

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.

Pathways for UNC 0642

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