UNC 0638

Pricing Availability Delivery Time Qty
Cat.No. 4343 - UNC 0638 | C30H47N5O2 | CAS No. 1255517-77-1
Description: Selective G9a and GLP inhibitor
Chemical Name: 2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Selective inhibitor of G9a and GLP histone lysine methyltransferases (IC50 values are < 15 nM and 19 nM for G9a and GLP respectively, and > 10000 nM for a range of other histone methyltransferases). Potently inhibits dimethylation of H3K9 in MCF-7 cells (IC50 = 70 nM). Cell permeable.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the UNC 0638 probe summary on the SGC website.

Compound Libraries

UNC 0638 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 509.73
Formula C30H47N5O2
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1255517-77-1
PubChem ID 46224516
InChI Key QOECJCJVIMVJGX-UHFFFAOYSA-N
Smiles CC(C)N(CC5)CCC5NC1=C2C(C=C(OCCCN4CCCC4)C(OC)=C2)=NC(C3CCCCC3)=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 50.97 100
DMSO 50.97 100
ethanol 50.97 100

Preparing Stock Solutions

The following data is based on the product molecular weight 509.73. 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 1.96 mL 9.81 mL 19.62 mL
5 mM 0.39 mL 1.96 mL 3.92 mL
10 mM 0.2 mL 0.98 mL 1.96 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Vedadi et al (2011) A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat.Chem.Biol. 7 566 PMID: 21743462

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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Keywords: G9a GLP histone lysine methyltransferases HMTs HMTases epigenetics histone modifications H3K9 H3K9me2 potent selective inhibits inhibitors UNC0638 Lysine Methyltransferases

Citations for UNC 0638

Citations are publications that use Tocris products.

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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 0638

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