| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 200mg | 电议 |
| 500mg | 电议 |
Cell lines |
Squamous cell carcinomas (SCC):A431 cells |
Preparation Method |
AZ1 was added to the medium of A431 cells for 48h |
Reaction Conditions |
15 μM, 48 h |
Applications |
USP25/28 inhibitor AZ1-mediated inhibition of USP28 led to changes as measured with predominant effects on pathways associated with cellular stress, cell cycle progression and DNA damage checkpoint and repair. An upregulation of DNA damage sensors like TP53BP1, MRE11 or RAD50 and simultaneously the downregulation of proteins involved in replication-coupled DNA repair, such as RAD51, RPA1 or RPA2. Of note, loss of USP28 activity was associated with a significant decrease of proteins involved in DNA replication. |
Animal models |
Usp25+/+and Usp25-/-mice(age-matched and sex-matched mice) |
Preparation Method |
At 12 weeks old, mice were injected with PBS or USP25/28 inhibitor AZ1 (40 mg per kg body weight) by gavage every 3 d for 8 weeks. |
Dosage form |
40 mg/kg, every 3 d for 8 weeks. |
Applications |
To test the effects of USP25/28 inhibitor AZ1 on DSS-induced colitis and found that USP25/28 inhibitor AZ1 gavage protected from weight loss and diarrhea and impaired colon shortening and potentiated the expression of proinflammatory cytokines and antibacterial peptides in colons. |
| 半岛bd体育手机客户端 描述 | USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. High expression levels of USP28 are essential for colon and breast cancers, and stabilization of c-Myc by USP28 is essential for tumor cell proliferation[5] USP25/28 inhibitor AZ1-mediated inhibition of USP28 led to changes as measured with predominant effects on pathways associated with cellular stress, cell cycle progression and DNA damage checkpoint and repair. An upregulation of DNA damage sensors like TP53BP1, MRE11 or RAD50 and simultaneously the downregulation of proteins involved in replication-coupled DNA repair, such as RAD51, RPA1 or RPA2[3] USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice mode[1].To test the effects of AZ1 on DSS-induced colitis and found that AZ1 gavage protected from weight loss and diarrhea and impaired colon shortening and potentiated the expression of proinflammatory cytokines and antibacterial peptides. In addition, levels of p-p65, p-p38 and SOCS3 were potentiated and levels of TRAF3 and pSTAT3 were decreased in colon tissues from AZ1-treated mice. In addition, gavage of AZ1 maintained weight gain and reduced the bacteria count in feces after C. rodentium infection. inflammation and bacterial replication in the colon were impaired, expression of proinflammatory cytokines and antibacterial peptides was potentiated, levels of p-p65 and p-p38 were increased and levels of TRAF3 were decreased in colons of mice with AZ1 gavage[2].Subchronic injection of AZ1 in 5 FAD mice markedly ameliorated memory deficits in cued FC and MWM tests.In addition, LTP impairment was reversed through long-term AZ1 administration.AZ1 administration attenuated microglial proliferation and activation in the hippocampusand cortex of 5×FAD mice.AZ1 ameliorated AD neuropathology by attenuating microglial activation[4] References: |
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