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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: ≥98% (HPLC)
Biological Activity for UNC 0638
UNC 0638 is a 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). Restores metabolic and antiviral function in exhausted CD8+ T cells from patients with chronic HCV infection. 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 for UNC 0638
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 for UNC 0638
UNC 0638 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for UNC 0638
| M. Wt | 509.73 |
| Formula | C30H47N5O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1255580-76-7 |
| 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 for UNC 0638
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.97 | 100 | |
| ethanol | 50.97 | 100 |
Preparing Stock Solutions for UNC 0638
The following data is based on the product molecular weight 509.73. 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 | 1.96 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 for UNC 0638
References for UNC 0638
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
Barili et al (2020) Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection. Nat.Commun. 11 604 PMID: 32001678
If you know of a relevant reference for UNC 0638, please let us know.
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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, chronic, infection, CD8+, T, cell, exhaustion, exhausted, Lysine, Methyltransferases, G9a/GLP, 4343, Tocris Bioscience
4 Citations for UNC 0638
Citations are publications that use Tocris products. Selected citations for UNC 0638 include:
Jen-Tsan et al (2020) G9a Promotes Breast Cancer Recurrence through Repression of a Pro-inflammatory Program. Cell Rep 33 108341 PMID: 33147463
Bellamy et al (2020) Increased Efficacy of Histone Methyltransferase G9a Inhibitors Against MYCN-Amplified Neuroblastoma. Front Oncol 10 PMID: 32537432
Mercè et al (2018) Loss of G9a preserves mutation patterns but increases chromatin accessibility, genomic instability and aggressiveness in skin tumours. Nat Cell Biol 20 1400-1409 PMID: 30455462
Elena et al (2019) Suppression of STING Associated with LKB1 Loss in KRAS-Driven Lung Cancer. Cancer Discov 9 34-45 PMID: 30297358
Do you know of a great paper that uses UNC 0638 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!
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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 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.