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Merck
CN

662142

DUB Inhibitor VI, P22077

The DUB Inhibitor VI, P22077 controls the biological activity of DUB. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

Synonym(s):

DUB Inhibitor VI, P22077, P022077, 1-(5-(2,4-Difluorophenylthio)-4-nitrothiophen-2-yl)ethanone, USP7 Inhibitor II, USP47 Inhibitor II, USP7 Inhibitor II, USP47 Inhibitor II, P022077, 1-(5-(2,4-Difluorophenylthio)-4-nitrothiophen-2-yl)ethanone

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About This Item

Empirical Formula (Hill Notation):
C12H7F2NO3S2
CAS Number:
Molecular Weight:
315.32
UNSPSC Code:
12352200
NACRES:
NA.28
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

off-white

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O

InChI key

RMAMGGNACJHXHO-UHFFFAOYSA-N

General description

A cell-permeable thiophenylethanone that is shown to inhibit USP7 and USP47 deubiquitinase activity (IC50 = 8.01 & 8.74 µM, respectively), while exhibiting much reduced affinity toward ATXN3, BAP1, and USP1, and displaying no inhibitory activity toward other known PR-619 (Cat. No. 662141) targets (IC50 >50 µM). Both P22077 and PR-619 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150 µM; 0.5 to 20 h), however PR619 treatment results in upregulation of both K48- and K63-linked, while P22077 exposure results in mainly enrichment of K48-linked polyUb chains.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Altun, M., et al. 2011. Chem. Biol.18, 1401.
Tian, X., et al. 2011. Assay Drug Dev. Technol.9, 165.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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