AZ1, USP25/28 inhibitor (TBI4317)

Description

Product Details

Formal Name: 2-[[5-Bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methylamino]ethanol

Molecular Formula: C₁₇H₁₆BrF₄NO₂

Formula Weight: 422.22

CAS Number: 2165322-94-9

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to greater than 18 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

USP25/28 inhibitor

Functions

Selective dual inhibitor of the deubiquitinases USP25 and 28 (IC₅₀’s = 620 nM and 700 nM respectively). It reduced c-Myc levels in HCT116, SW480, and HT29 colon cancer cell lines. AZ1 inhibited SARS-CoV-2 replication in Vero E6 cells. It caused DNA damage, promoted c-Myc degradation, and induced apoptosis in non-small cell lung cancer cells alone and in combination with cisplatin. Treatment of chronic lymphocytic leukemia cells with AZ1 suppressed Notch activation and reduced cell viability in combination with venetoclax. It reduced c-Myc expression in clear cell renal cell carcinoma leading to tumor growth suppression. AZ1 ameliorated Parkinson’s disease via USP25-dependent restoration of mitophagy.

Application Procedures

First dissolved in DMSO (up to greater than 18 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4317_AZ1_Datasheet

MSDS:

TBI4317_AZ1_MSDS

Research use only.