USP25/28 inhibitor AZ1

SKU: orb1299594

Description

AZ1 is a selective, orally bioavailable, non-competitive dual inhibitor of ubiquitin-specific proteases USP25 and USP28, with IC50 values of 0.7 µM and 0.6 µM, respectively. This compound demonstrates anti-inflammatory and anti-tumor activities in research models, supporting its investigation in oncology and immunology.

Research Area

Cell Biology, Molecular Biology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 2165322-94-9
• MW: 422.21
• Purity: 99.79% (May vary between batches)
• Formula: C₁₇H₁₆BrF₄NO₂
• SMILES: OCCNCc1cc(Br)ccc1OCc1ccc(F)c(c1)C(F)(F)F
• Target: DUB
• Solubility: DMSO:250 mg/mL (592.12 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.84 mM)

Bioactivity

• Target IC50:
  USP25:0.7 nM |USP28:0.6 nM
• In Vivo:
  Method: USP25/28 inhibitor AZ1 (AZ1) (20, 40mg/kg, gavage) was given to WT Model mice were used to study the effect of USP25/28 inhibitor AZ1 (AZ1) on DSS-induced colitis. RESULTS USP25/28 inhibitor AZ1 (AZ1) treatment significantly reduced the number of colon tumors; the expression of wnt-related genes and pSTAT3 levels in tumors in the USP25/28 inhibitor AZ1 (AZ1) treatment group were reduced, and the SOCS3 level was increased; USP25/28 inhibitor Inflammation and bacterial replication were impaired in the colon of mice gavaged with AZ1 (AZ1), the expression of pro-inflammatory cytokines and antimicrobial peptides was enhanced, p-p65 and p-p38 levels were increased, and TRAF3 levels were decreased.
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• In Vitro:
  METHODS: HCT116 cells were treated with USP25/28 inhibitor AZ1 (20, 40, 60, 80, 100 μM) and samples were collected 3 hours later for Western blot analysis of USP28, c-Myc and PARP. RESULTS Western blot analysis showed that the total protein level of c-Myc decreased rapidly and concentration-dependently after treatment with USP25/28 inhibitor AZ1.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

USP25/28, USP25/28 inhibitor AZ1, USP-25/28 inhibitor AZ1, Deubiquitinase, DUBs, AZ1, AZ-1, AZ 1

Compound Identifiers

PubChem CID

135397656