UNC 0646

G9a and GLP inhibitor CAS# 1320288-17-2

UNC 0646

Catalog No. BCC2431----Order now to get a substantial discount!

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UNC 0646: 5mg $69 In Stock
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Chemical structure

UNC 0646

3D structure

Chemical Properties of UNC 0646

Cas No. 1320288-17-2 SDF Download SDF
PubChem ID 53315882 Appearance Powder
Formula C36H59N7O2 M.Wt 621.9
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 33.33 mg/mL (53.59 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name N-(1-cyclohexylpiperidin-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)-2-(4-propan-2-yl-1,4-diazepan-1-yl)quinazolin-4-amine
SMILES CC(C)N1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)C5CCCCC5)OC)OCCCN6CCCCC6
Standard InChIKey OUKWLRHRXOPODD-UHFFFAOYSA-N
Standard InChI InChI=1S/C36H59N7O2/c1-28(2)41-19-10-20-43(24-23-41)36-38-32-27-34(45-25-11-18-40-16-8-5-9-17-40)33(44-3)26-31(32)35(39-36)37-29-14-21-42(22-15-29)30-12-6-4-7-13-30/h26-30H,4-25H2,1-3H3,(H,37,38,39)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of UNC 0646

DescriptionPotent 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.

UNC 0646 Dilution Calculator

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UNC 0646 Molarity Calculator

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Preparing Stock Solutions of UNC 0646

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.608 mL 8.0399 mL 16.0798 mL 32.1595 mL 40.1994 mL
5 mM 0.3216 mL 1.608 mL 3.216 mL 6.4319 mL 8.0399 mL
10 mM 0.1608 mL 0.804 mL 1.608 mL 3.216 mL 4.0199 mL
50 mM 0.0322 mL 0.1608 mL 0.3216 mL 0.6432 mL 0.804 mL
100 mM 0.0161 mL 0.0804 mL 0.1608 mL 0.3216 mL 0.402 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on UNC 0646

IC50: 6 nm (G9a IC50); 26 nm (Cellular IC50); 3.3 μM (Cell toxicity EC50)

Histone-lysine N-methyltransferase, H3 lysine-9 specific 3, also known as euchromatic histone-lysine N-methyltransferase 2 (EHMT2) and G9a, is a histone methyltransferase that in humans is encoded by the EHMT2 gene. Protein lysinemethyltransferase G9a plays key roles in the transcriptional repression of a variety of genes via dimethylation of lysine 9 on histoneH3 (H3K9me2) of chromatin as well as dimethylation of nonhistone proteins including tumor suppressor p53.

In vitro: UNC0646 is reported to be 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). UNC0646 also potently blocks G9a/GLP methyltransferase activity in cells (IC50 = 10 nM in MCF7 cells) and exhibits low cellular toxicity (EC50 = 4.7 μM in MCF7 cells). UNC0646 is selective for G9a/GLP over a range of other protein lysine methyltransferases and protein arginine methyltransferases [1].

In vivo: The authors previously discovered potent and selective G9a/GLP inhibitors including the cellular chemical probe UNC0638, which displays an excellent separation of functional potency and cell toxicity. However, this inhibitor is not suitable for animal studies due to its poor pharmacokinetic (PK) properties. In this study, the authors report the discovery of the first G9a and GLP in vivo chemical probe UNC0642, which not only maintains high in vitro and cellular potency, low cell toxicity, and excellent selectivity, but also displays improved in vivo PK properties, making it suitable for animal studies [2].

References:
[1] Liu F, Barsyte-Lovejoy D, Allali-Hassani A, He Y, Herold JM, Chen X, Yates CM, Frye SV, Brown PJ, Huang J, Vedadi M, Arrowsmith CH, Jin J.  Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011;54(17):6139-50.
[2] Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh V, Huang XP, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J.  Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013;56(21):8931-42.

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References on UNC 0646

Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.[Pubmed:21780790]

J Med Chem. 2011 Sep 8;54(17):6139-50.

Protein lysine methyltransferase G9a plays key roles in the transcriptional repression of a variety of genes via dimethylation of lysine 9 on histone H3 (H3K9me2) of chromatin as well as dimethylation of nonhistone proteins including tumor suppressor p53. We previously reported the discovery of UNC0321 (3), the most potent G9a inhibitor to date, via structure-based design and structure-activity relationship (SAR) exploration of the quinazoline scaffold represented by BIX01294 (1). Despite its very high in vitro potency, compound 3 lacks sufficient cellular potency. The design and synthesis of several generations of new analogues aimed at improving cell membrane permeability while maintaining high in vitro potency resulted in the discovery of a number of novel G9a inhibitors such as UNC0646 (6) and UNC0631 (7) with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity. The design, synthesis, and cellular SAR of these potent G9a inhibitors are described.

Description

UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM.

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