UNC 0638

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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)
Citations (4)
Literature (2)

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

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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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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View all G9a/GLP Inhibitors

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:

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

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

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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Epigenetics Scientific Review

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

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.