IndraLab

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ML323 inhibits USP1. 15 / 15
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"USP1 inhibition by ML323 promoted fracture healing in nonunion rats and facilitated the expression of osteogenesis-related factors and the signaling of PI3K/Akt pathway."
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"ML323 inhibits Usp1 with a Ki of less than 100 nM and is highly selective for Usp1 , as determined by in vitro assays and DUB profiling in cells ."
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"Notably, ML323 did not disrupt the association of the USP1 and UAF1 subunits in the complex."
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"Using HA tagged Ub-VME, which has been used to profile DUB activity in cell lysates XREF_BIBR, XREF_BIBR, we showed that ML323 efficiently inhibited the labeling of USP1 by the Ub-VME probe and exhibited selectivity toward other DUBs in human cells."
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"USP1 inhibition by ML323 at two concentrations (5 and 10 muM), which proved to be non toxic at basal levels (data not shown), potently inhibited the induction of caspase-3 and PARP cleavage triggered [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The exact cause of this discrepancy is not clear; however, given that ML323 only inhibits the DUB activity of USP1 without changing the USP1 protein level in treated cells, such a difference may suggest a structural role of USP1 or USP1-UAF1 in FANCD2 foci formation."
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"Here, we further show that ML323 treatment also prevents USP1 autocleavage, causing increased numbers of USP1 molecules to become inadvertently trapped on DNA."
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"Combination treatment of enzalutamide and targeting KDM4A stabilization through pharmacological inhibition of USP1 by ML323 could thus open an avenue for therapeutic intervention in PC patients ."
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"Pharmacological inhibition of USP1 by ML323 exhibited cell cytotoxicity in human T-ALL cells."
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"ML323 inhibits Usp1 with a K i of less than 100 nM and is highly selective for Usp1, as determined by in vitro assays and DUB profiling in cells."
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"ML323 was able to potently inhibit USP1 activity in a dose dependent manner in several complementary in vitro assays as well as in cellular models as represented by increased monoubiquitination of USP[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In contrast, inhibition of USP1 by ML323 decreased the I-SceI-induced HR frequency to 0.81% (XREF_FIG and XREF_SUPPLEMENTARY)."
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"Inhibition of USP1 was also confirmed in INS-1E cells treated with ML323 as indicated by the accumulation of ubiquitinated PCNA, a USP1 downstream substrate."
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"A chemical inhibitor of USP1, ML323, has been developed that showed promise in inducing cytotoxicity in cisplatin-treated non-small lung cancers and osteosarcoma cells 56 ."
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"Targeting KDM4A stabilization through pharmacological inhibition of USP1 by ML323 could thus open an avenue for therapeutic intervention in prostate cancer patients ."
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