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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)
Biological Activity for UNC 0646
UNC 0646 is a 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.
Technical Data for UNC 0646
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for UNC 0646
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 62.19 | 100 | |
| ethanol | 62.19 | 100 |
Preparing Stock Solutions for UNC 0646
The following data is based on the product molecular weight 621.9. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 1.61 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 |
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Product Datasheets for UNC 0646
References for UNC 0646
References are publications that support the biological activity of the product.
Liu et al (2011) Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J.Med.Chem. 54 6139 PMID: 21780790
If you know of a relevant reference for UNC 0646, please let us know.
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Keywords: UNC 0646, UNC 0646 supplier, UNC0646, epigenetics, SGC, G9a, GLP, histone, protein, lysine, methyltransferases, PKMTs, HMTs, potent, selective, inhibitors, inhibits, Lysine, Methyltransferases, G9a/GLP, 4342, Tocris Bioscience
Citations for UNC 0646
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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* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cancer Research Product Guide
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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 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:
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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.