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Merck

662143-M

DUB Inhibitor XI

Synonym(s):

4-Cyano-5-((3,5-dichloropyridin-4-yl)thio)-N-(4-(methylsulfonyl)phenyl)thiophene-2-carboxamide, USP47 Inhibitor III, USP7 Inhibitor III

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About This Item

UNSPSC Code:
41121800
NACRES:
NA.77
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assay

≥95% (HPLC)

Quality Segment

form

solid

packaging

pkg of 10 mg

shipped in

ambient

storage temp.

2-8°C

General description

A cell-permeable dichloropyridinylthio-thiophenecarboxamide that is more potent than DUB Inhibitor VI, P22077 (Cat. No. 662142) as a dual inhibitor against USP7 (IC50 = 0.42 vs. 8.0 µM with respective inhibitor) and USP47 (IC50 = 1.0 vs. 8.7 µM with respective inhibitor), while exhibiting comparable cytotoxicity toward HCT-116 (CC50 = 7.6 vs. 7.8 µM with respective inhibitor) by upregulating cellular p21 and p53 protein levels in a time-dependent manner. Displays little potency against USP2, USP5, USP8, USP21 USP28, cathepsin B, caspase-3, calpain-1, or 20S proteasome chymotrypsin-like activity (IC50 >31.6 µM).


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

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