DUBs-IN-2deubiquitinase enzyme inhibitor CAS# 924296-19-5 |
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Quality Control & MSDS
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| Cas No. | 924296-19-5 | SDF | Download SDF |
| PubChem ID | 16065491 | Appearance | Powder |
| Formula | C15H9N5O | M.Wt | 275.26 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 9.06 mg/mL (32.91 mM; Need ultrasonic and warming) | ||
| Chemical Name | (9E)-9-ethoxyiminoindeno[1,2-b]pyrazine-2,3-dicarbonitrile | ||
| SMILES | CCON=C1C2=CC=CC=C2C3=NC(=C(N=C31)C#N)C#N | ||
| Standard InChIKey | VKVAJBRQGBRHIK-XSFVSMFZSA-N | ||
| Standard InChI | InChI=1S/C15H9N5O/c1-2-21-20-14-10-6-4-3-5-9(10)13-15(14)19-12(8-17)11(7-16)18-13/h3-6H,2H2,1H3/b20-14+ | ||
| 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. |
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| 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. |
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| 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. | ||
| Description | DUBs-IN-2 is a potent deubiquitinase inhibitor with an IC50 of 0.28 μM for USP8.In Vitro:DUBs-IN-2 (compound 22 e) is a potent USP8 inhibitor with an IC50 of 0.28 μM, and has no effect on USP7, with an IC50 of >100 μM. DUBs-IN-2 inhibits the viability of HCT116 colon cell line and PC-3 prostate cancer cell line with IC50 values of 0.5-1.5 μM[1]. References: | |||||
DUBs-IN-2 Dilution Calculator
DUBs-IN-2 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.6329 mL | 18.1646 mL | 36.3293 mL | 72.6586 mL | 90.8232 mL |
| 5 mM | 0.7266 mL | 3.6329 mL | 7.2659 mL | 14.5317 mL | 18.1646 mL |
| 10 mM | 0.3633 mL | 1.8165 mL | 3.6329 mL | 7.2659 mL | 9.0823 mL |
| 50 mM | 0.0727 mL | 0.3633 mL | 0.7266 mL | 1.4532 mL | 1.8165 mL |
| 100 mM | 0.0363 mL | 0.1816 mL | 0.3633 mL | 0.7266 mL | 0.9082 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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IC50s: 7.2 M/0.93 M for USP7/USP8, respectively.
DUBs-IN-2 is a potent deubiquitinase enzyme inhibitor.
USP7 (or HAUSP) associated with the protein Mdm2 (an E3 ubiquitin ligase) recognizes the N-terminal transactivation domain of the p53 tumor suppressor and elicites its degradation by ubiquitination. USP7 also interacts with directly essential viral proteins (p53, FOXO4, PTEN) and oncogenic pathways. In addition, phenotypes connected with USP7 silencing strongly reveal that targeting USP7 by small-molecule inhibitors may be an potential direction for antiviral and anticancer therapies. USP8 (or UBPY) interacts with many substrates, such as the epidermal growth factor receptor (EGFR), an essential for the regulating cell survival, proliferation, and differentiation pathways), and is a critical regulator of receptor endocytosis and trafficking [1].
In vitro: Human USP7 and USP8 enzymes in baculovirus-infected insect cells were overexpressed in their full-length forms, then purified by the His-tag affinity chromatography procedure. using ubiquitin C-terminal 7-amido-4-methylcoumarin (Ub–AMC) evaluates inhibition of USP7 and USP8 deubiquitinating activity. Ub–AMC is hydrolyzed by deubiquitinating enzymes, thus releasing AMC. IC50 values were calculated based on dose–response curve after dilution of this compound in eight final concentrations, ranging from 100 mm to 10 nm [1].
DUBs-IN-2 as potent inhibitors of USP7 and USP8 deubiquitinating enzymes was identified functionalized cyanopyrazines by high-throughput screening of 65092 chemically diverse compounds for activity toward full-length USP7 cysteine protease in a fluorescence-based biochemical assay [1].
In vivo: So far, no study in vivo has been conducted.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Colombo M, Vallese S, Peretto I, Jacq X, Rain JC, Colland F, Guedat P. Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes. ChemMedChem. 2010 Apr 6;5(4):552-8.
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