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Description: Potent and selective G9a and GLP inhibitor
Chemical Name: 2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
Purity: ≥99% (HPLC)
Biological Activity for UNC 0642
UNC 0642 is a potent and selective G9a and GLP histone lysine methyltransferase inhibitor (IC50 < 2.5 nM) that exhibits >2,000-fold selectivity for G9a and GLP over PRC2-EZH2 and >20,000-fold selectivity over other methyltransferases. UNC 0642 reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50 = 110 nM), and displays modest brain penetration in vivo.
Licensing Information
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.
External Portal Information for UNC 0642
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.
Compound Libraries for UNC 0642
UNC 0642 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for UNC 0642
| M. Wt | 546.7 |
| Formula | C29H44F2N6O2 |
| Storage | Store at -20°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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for UNC 0642
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.67 | 100 | |
| 1eq. HCl | 27.34 | 50 |
Preparing Stock Solutions for UNC 0642
The following data is based on the product molecular weight 546.7. 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 | 1.83 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 |
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Product Datasheets for UNC 0642
References for UNC 0642
References are publications that support the biological activity of the product.
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
Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761
If you know of a relevant reference for UNC 0642, please let us know.
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Keywords: UNC 0642, UNC 0642 supplier, UNC0642, potent, selective, G9a, GLP, histone, lysine, methyltransferase, inhibits, inhibitors, HMTs, HMTases, epigenetics, modifications, H3K9, H3K9me2, sgc, Lysine, Methyltransferases, G9a/GLP, 5132, Tocris Bioscience
3 Citations for UNC 0642
Citations are publications that use Tocris products. Selected citations for UNC 0642 include:
Bellamy et al (2020) Increased Efficacy of Histone Methyltransferase G9a Inhibitors Against MYCN-Amplified Neuroblastoma Front Oncol 10 PMID: 32537432
Xi et al (2022) EHMT2 methyltransferase governs cell identity in the lung and is required for KRAS G12D tumor development and propagation. Elife 11 PMID: 35983994
Xin et al (2019) Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell 176 1113-1127.e16 PMID: 30712867
Do you know of a great paper that uses UNC 0642 from Tocris? Please let us know.
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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.
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 in Cancer Poster
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.