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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.
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.
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.
UNC 0642 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
| 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.
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 27.34 | 50 | |
| DMSO | 54.67 | 100 |
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.
| 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 |
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
Keywords: UNC 0642, supplier, UNC0642, potent, selective, G9a, GLP, histone, lysine, methyltransferase, inhibits, inhibitors, HMTs, HMTases, epigenetics, modifications, H3K9, H3K9me2, sgc, Lysine, Methyltransferases, Lysine, Methyltransferases, Lysine, Methyltransferases, Tocris Bioscience
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