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Submit ReviewAZ1 USP25/28 inhibitor
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)
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.
| 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
If you know of a relevant reference for AZ1 USP25/28 inhibitor, please let us know.
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Keywords: AZ1 USP25/28 inhibitor, AZ1 USP25/28 inhibitor supplier, USP25, USP28, inhibitors, inhibits, selective, deubiquitinating, enzymes, c-Myc, Alzheimer's, disease, amyloid, neuroinflammation, Deubiquitinating, Enzymes, 7845, Tocris Bioscience
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