IndraLab

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WP1130 inhibits USP14. 16 / 16
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"Moreover, WP1130, which is found to be a partially selective DUB inhibitor, directly inhibits DUB activity of USP9x, USP5 and USP14 XREF_BIBR - XREF_BIBR."

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"In Z138 mantle cell lymphoma cells, WP1130 inhibits USP9x, USP5, USP14, UCH37, UCH-L1, and potentially other DUBs XREF_BIBR."

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"It was found that WP1130 can directly inhibit USP9X as well as DUBs of UCHL5, and USP14."

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"Four independent experiments demonstrated that WP1130 treatment significantly reduced USP14 activity in both mock- and virally infected samples compared to DMSO, but not compared to each other (XREF_FIG, quantitation)."

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"WP1130, on the other hand, inhibits at least five DUBs : USP5, UCH-L1, USP9X, USP14, and UCH37, and induces the cellular accumulation of polyubiquitinated proteins [XREF_BIBR]."

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"WP1130 (Degrasyn) has been shown to inhibit USP14 and UCHL5 as well as other DUB enzymes (see below)."

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"We hypothesized that inhibition of USP14 by WP1130 would result in IRE1 activation, one of the three sensors of the UPR XREF_BIBR."

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"WP1130 acts as a partly selective DUB inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37, which are known to regulate survival protein stability and 26S proteasome function."

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"For example, a general DUB inhibitor WP1130 has been known to inhibit the activities of USP9x, USP5, USP14 and UCH37 that regulate the survival proteins stability [XREF_BIBR]."

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"b-AP15 is a proteasomal DUBs inhibitor that blocks USP14 and UCHL5, which are also inhibited by WP1130."

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"WP1130 inhibits USP9X, USP5, USP14, UCH37, UCH-L1 in lymphoma cells, and potentially other DUBs as well XREF_BIBR."

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"Taken together, these results demonstrated that USP14 activity is inhibited by WP1130 in RAW cells without affecting total protein levels, and that USP14 activity and WP1130 inhibition of this activity is independent of viral infection."

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"For example , 8-mercapto-N - ( ( tetrahydro-3-furanyl ) methyl ) -4 - quinoline carboxamide , LND-57444 , VLX1570 , ML323 , ( ADC-01 , ADC-03 , HBX41108 , HBX19818 , P5091 , P22077 ) , 9 - ( ethoxyimino ) -9 H-indeno ( 1,2 - b ) pyrazine-2 ,3 - dicarbonitrile , WP1130 , Mitoxantrone and GSK2643943A are able to inhibit PSMD14 , UCHL1 , UCHL5 and USP14 , USP1 , USP7 , USP8 , USP9X , USP11 and USP20 , respectively ."

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"These data and the fact that UCH37 or USP14 may have a redundant DUB function and also that b-AP15 and WP1130 inhibit both UCH37 and USP14 suggests that a contribution from both enzymes may be needed."

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"WP1130, an inhibitor of DUBs, can suppress the activities of USP9X, USP5, USP14 and UCH37, deregulate anti-apoptotic protein MCL-1 and upregulate pro apoptotic protein p53."

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"WP1130 acts as a partly selective deubiquitinase inhibitor, directly inhibiting deubiquitinase activity of USP9X, USP5, USP14, and UCH37, which are known to regulate survival protein stability and 26S proteasome function."