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P22077 is a potent and selective ubiquitin-specific protease 7 (USP7) inhibitor. P22077 potently induces apoptosis in NB cells with an intact USP7-HDM2-p53 axis but not in NB cells with mutant p53 or without human homolog of MDM2 (HDM2) expression. P22077 was found to be able to sensitize chemoresistant LA-N-6 NB cells to chemotherapy. In an in vivo orthotopic NB mouse model, P22077 significantly inhibited the xenograft growth of three NB cell lines. USP7-specific inhibitors like P22077 may serve not only as a stand-alone therapy but also as an effective adjunct to current chemotherapeutic regimens for treating NB with an intact USP7-HDM2-p53 axis. Synonyms: P-22077; P 22077. Grades: 0.98. CAS No. 1247819-59-5. Molecular formula: C12H7F2NO3S2. Mole weight: 315.309.
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. Group: Fluorescence/luminescence spectroscopy.
A cell-permeable thiophenylethanone that is shown to inhibit USP7 and USP47 deubiquitinase activity (IC50=8.01 & 8.74uM, respectively), while exhibiting much reduced affinity toward ATXN3, BAP1, and USP1, and displaying no inhibitory activity toward other known PR-619 targets (IC50 >50uM). Both P22077 and PR-619 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150uM; 0.5 to 20h), however PR619 treatment results in upregulation of both K48- and K63-linked, while P22077 exposure results in mainly enrichment of K48-linked polyUb chains. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences.
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DUB Inhibitor V, PR-619
A cell-permeable pyridinamine class broad-spectrum DUB inhibitor whose known targets include ATXN3, BAP1, JOSD2, OTUD5, UCH-L1, UCH-L3, UCH-L5/UCH37, USP1, 2, 4, 5, 7, 8, 9X, 10, 14, 15, 16, 19, 20, 22, 24, 28, 47, 48, VCIP135, YOD1, as well as deISGylase PLpro, deNEDDylase DEN1, and deSUMOlyase SENP6. Both PR-619 and P22077 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150uM; 0.5 to 20h), however P22077 exposure results in mainly enrichment of K48-linked, while PR619 treatment results in upregulation of both K48- and K63-linked polyUb chains. Group: Biochemicals. Alternative Names: PR619; UCH-L1 Inhibitor IV; UCH-L3 Inhibitor II; UCH-L5/UCH37 Inhibitor III; USP5 Inhibitor II; USP7 Inhibitor I; USP9X Inhibitor II; USP14 Inhibitor IV; USP14 Inhibitor IV; USP47 Inhibitor I; 2,6-Diaminopyridine-3,5-bis(thiocyanate); 3,5-Dithiocyanatopyridine-2,6-diamine. Grades: Highly Purified. CAS No. 21645-32-1. Pack Sizes: 25mg. Molecular Formula: C?H?N?S?, Molecular Weight: 223.3. US Biological Life Sciences.
Worldwide
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