AZ1 USP25/28 inhibitor

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Description: Selective USP25 and USP28 inhibitor
Chemical Name: 2-[[[5-Bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]ethanol
Purity: ≥98% (HPLC)
Datasheet
Citations
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Biological Activity for AZ1 USP25/28 inhibitor

AZ1 USP25/28 inhibitor is a selective inhibitor of USP28 (IC50 = 0.6 μM, Kd= 0.2 - 3.7 μM) and USP25 (IC50 = 0.7 μM). AZ1 USP25/28 inhibitor exhibits selectivity for USP25 and USP28 over other DUB family members. The compound dose-dependently reduces c-Myc levels in colon carcinoma cells in vitro and induces cell death (EC50 values are 18 - 20 μM). In a mouse Alzheimer's disease model, AZ1 USP25/28 inhibitor reduces amyloid burden, attenuates microglial activation and improves synaptic and cognitive function.

Technical Data for AZ1 USP25/28 inhibitor

M. Wt 422.21
Formula C17H16BrF4NO2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2165322-94-9
PubChem ID 135397656
InChI Key ITHSFXDGKQYOED-UHFFFAOYSA-N
Smiles FC1=CC=C(COC2=CC=C(C=C2CNCCO)Br)C=C1C(F)(F)F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AZ1 USP25/28 inhibitor

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 42.22 100

Preparing Stock Solutions for AZ1 USP25/28 inhibitor

The following data is based on the product molecular weight 422.21. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.37 mL 11.84 mL 23.68 mL
5 mM 0.47 mL 2.37 mL 4.74 mL
10 mM 0.24 mL 1.18 mL 2.37 mL
50 mM 0.05 mL 0.24 mL 0.47 mL

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Product Datasheets for AZ1 USP25/28 inhibitor

References for AZ1 USP25/28 inhibitor

References are publications that support the biological activity of the product.

Wrigley et al (2017) Identification and characterization of dual inhibitors of the USP25/28 deubiquitinating enzyme subfamily. ACS Chem.Biol. 12 3113 PMID: 29131570

Zheng et al (2021) Trisomy 21-induced dysregulation of microglial homeostasis in Alzheimer's brains is mediated by USP25. Sci.Adv. 7 eabe1340 PMID: 33523861

Zheng et al (2022) USP25 inhibition ameliorates Alzheimer's pathology through the regulation of APP processing and Aβ generation. J.Clin.Invest. 132 e152170 PMID: 35229730


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Citations for AZ1 USP25/28 inhibitor

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