IndraLab

Statements

WP1130 inhibits UCHL5. 17 / 17
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"Assessment of DUB activity using recombinant proteins and in cell-based assays revealed that WP1130 inhibits USP5, USP9X, USP14, and UCH37, but not UCHL3."
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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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"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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"In Z138 mantle cell lymphoma cells, WP1130 inhibits USP9x, USP5, USP14, UCH37, UCH-L1, and potentially other DUBs XREF_BIBR."
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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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"In contrast, WP1130 is a specific inhibitor of USP5, 9X, 14, 37, and UCHL5."
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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."
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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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"These findings indicate that PR-619 inhibits DUB action independently of MSK1, but WP1130 inhibits DUB action, which is essential for MSK1 to increase Snail protein expression.While PR-619 is a general DUB inhibitor that inhibits many DUBs, WP1130 inhibits a subgroup of DUBs, including UCHL1, UCHL5, USP5, USP9X and USP14 (ref."
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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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"b-AP15 is a proteasomal DUBs inhibitor that blocks USP14 and UCHL5, which are also inhibited by WP1130."
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"Although WP1130 is thought to inhibit other DUBs (USP5, USP14, UCH37 and UCH-L1) , the orthologous Drosophila genes were either not identified as hits in our in vivo RNAi screen or had the opposite effect to Faf, suggesting that Faf is the relevant target for WP1130 in the context of Ft regulation.However, whilst the DUB activity of Faf seems to be required for the regulation of Ft protein levels and function, it is still unclear whether Faf directly deubiquitylates Ft or if its effect is indirect."
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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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"However, we found that several reported DUB inhibitors, including WP1130 (a known inhibitor of USP5, USP9X, USP14, USP24, and UCH37, Figure 4B), inhibit USP18 protease activity in an ISG15-Rho assay (Figure S8)."
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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 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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