UNC 0638

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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
Reviews
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.

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 UNC 0638 is reviewed on the chemical probes 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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.97 100
ethanol 50.97 100
1eq. HCl 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.

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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References

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

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: UNC 0638, UNC 0638 supplier, G9a, GLP, histone, lysine, methyltransferases, HMTs, HMTases, epigenetics, modifications, H3K9, H3K9me2, potent, selective, inhibits, inhibitors, UNC0638, Lysine, Methyltransferases, G9a/GLP, 4343, Tocris Bioscience

Citations for UNC 0638

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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!

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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.