UNC 0646

Pricing Availability Delivery Time Qty
Cat.No. 4342 - UNC 0646 | C36H59N7O2 | CAS No. 1320288-17-2
Description: Potent and selective G9a and GLP inhibitor
Chemical Name: N-(1-Cyclohexyl-4-piperidinyl)-2-[hexahydro-4-(1-methylethyl)-1H-1,4-diazepin-1-yl]-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50 values are 6 nM and 15 nM for G9a and GLP, respectively). Potently blocks G9a/GLP methyltransferase activity in cells (IC50 = 10 nM in MCF7 cells); exhibits low cellular toxicity (EC50 = 4.7 μM in MCF7 cells). Selective for G9a/GLP over a range of other protein lysine methyltransferases and protein arginine methyltransferases.

Compound Libraries

UNC 0646 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 621.9
Formula C36H59N7O2
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1320288-17-2
PubChem ID 53315882
InChI Key OUKWLRHRXOPODD-UHFFFAOYSA-N
Smiles CC(C)N(CC6)CCCN6C1=NC(NC3CCN(C5CCCCC5)CC3)=C2C(C=C(OCCCN4CCCCC4)C(OC)=C2)=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 62.19 100
ethanol 62.19 100

Preparing Stock Solutions

The following data is based on the product molecular weight 621.9. 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 1.61 mL 8.04 mL 16.08 mL
5 mM 0.32 mL 1.61 mL 3.22 mL
10 mM 0.16 mL 0.8 mL 1.61 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

Molarity Calculator

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Liu et al (2011) Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J.Med.Chem. 54 6139 PMID: 21780790


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View all Lysine Methyltransferase Inhibitors

Keywords: UNC0646 epigenetics SGC G9a GLP histone protein lysine methyltransferases PKMTs HMTs potent selective inhibitors inhibits Lysine Methyltransferases

Citations for UNC 0646

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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 0646

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