| DUBs-IN-2deubiquitinase enzyme inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
DUBs-IN-2 Dilution Calculator
calculate
DUBs-IN-2 Molarity Calculator
calculate
| Cas No. | 924296-19-5 | SDF | Download SDF |
| Chemical Name | (E)-9-(ethoxyimino)-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile | ||
| Canonical SMILES | CCO/N=C1C2=CC=CC=C2C3=C1N=C(C(C#N)=N3)C#N | ||
| Formula | C15H9N5O | M.Wt | 275.26 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| 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. | ||
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.
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
>
个人感觉这个就是厂家的一个噱头，，，听说有人已经在无抗猪肉中发现抗药性细菌，不知是真是假，不过要买的话一定要去信誉的地方。
以上回答，希望对你有用。
