AZ-1
- Product Name
- AZ-1
- CAS No.
- 2165322-94-9
- Chemical Name
- AZ-1
- Synonyms
- USP25/28 inhibitor AZ1;USP25 and 28 inhibitor AZ-1;AZ-1;AZ-1;AZ 1;AZ1;AZ1 USP25/28 inhibitor;USP25/28 inhibitor AZ1, 10 mM in DMSO;2-((5-bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)benzyl)amino)ethanol;2-((5-Bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)benzyl)amino)ethan-1-ol;Ethanol, 2-[[[5-bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]-;Deubiquitinase,USP-25/28 inhibitor AZ1,USP25/28 inhibitor AZ1,inhibit,AZ 1,Inhibitor,AZ-1,DUBs
- CBNumber
- CB44668637
- Molecular Formula
- C17H16BrF4NO2
- Formula Weight
- 422.21
- MOL File
- 2165322-94-9.mol
AZ-1 Property
- Boiling point:
- 478.5±40.0 °C(Predicted)
- Density
- 1.488±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: ≥ 250 mg/mL (592.12 mM); Water: < 0.1 mg/mL (insoluble)
- pka
- 14.74±0.10(Predicted)
- form
- Solid
- color
- White to off-white
- InChI
- InChI=1S/C17H16BrF4NO2/c18-13-2-4-16(12(8-13)9-23-5-6-24)25-10-11-1-3-15(19)14(7-11)17(20,21)22/h1-4,7-8,23-24H,5-6,9-10H2
- InChIKey
- ITHSFXDGKQYOED-UHFFFAOYSA-N
- SMILES
- C(O)CNCC1=CC(Br)=CC=C1OCC1=CC=C(F)C(C(F)(F)F)=C1
N-Bromosuccinimide Price
- Product number
- CS-0065552
- Product name
- USP25/28inhibitorAZ1
- Purity
- 98.10%
- Packaging
- 5mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- CS-0065552
- Product name
- USP25/28inhibitorAZ1
- Purity
- 98.10%
- Packaging
- 10mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-0065552
- Product name
- USP25/28inhibitorAZ1
- Purity
- 98.10%
- Packaging
- 25mg
- Price
- $500
- Updated
- 2021/12/16
- Product number
- CS-0065552
- Product name
- USP25/28inhibitorAZ1
- Purity
- 98.10%
- Packaging
- 50mg
- Price
- $850
- Updated
- 2021/12/16
- Product number
- CS-0065552
- Product name
- USP25/28inhibitorAZ1
- Purity
- 98.10%
- Packaging
- 100mg
- Price
- $1450
- Updated
- 2021/12/16
AZ-1 Chemical Properties,Usage,Production
Uses
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. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model[1][2].
Biological Activity
AZ1 is a potent and selective dual USP25 & USP28 deubiquitinase (DUBs) inhibitor (USP25/28 IC50 = 0.62/0.7 nM by Ub-Rh110 assay) th at induces HCT116 cellular c-Myc degradation (20-100 μM for 3h or 60 μM for 0.3-3h). AZ1 exhibits antiproliferation activity in cancer cultures (IC50 ≤20 μM; HCT116, HT29 and SW480) and anti-tumor efficacy in an orthotopic model of lung SCC tumours in mice in vivo (125 mg/kg or 375 mg/kg i.p. once every three days, 6 injections total).
in vivo
USP25/28 inhibitor AZ1 (AZ1; 40?mg/kg; gavage; daily; for 7?days) protects from dextran sulfate sodium (DSS)-induced weight loss and diarrhea and impaired colon shortening[1].
USP25/28 inhibitor AZ1 (20?mg/kg/day; gavage; 6 times a week in the 1, 3, 6 weeks) treatment significantly reduces tumor numbers in colons. Expression of Wnt-related genes and levels of pSTAT3 are decreased and levels of SOCS3 are increased in tumors. AZ1 gavage does not alleviate DSS-induced colitis in Usp25-/- mice or the spontaneous colitis of Il10-/- mice[1].
USP25/28 inhibitor AZ1 (20?mg/kg/day; gavage; every 3?days from 13-20 weeks) significantly inhibits tumorigenesis in the colon and prolonged the survival of AOM/Vil-Cre;Trp53fl/fl (VP) mice. AZ1 treatment has minimal effect on tumorigenesis in the USP25-deficient background[1].
| Animal Model: | 12-week old male Usp25+/+ and Usp25-/- mice[1] |
| Dosage: | 40?mg/kg |
| Administration: | Gavage; daily; for 7?days |
| Result: | Protected from dextran sulfate sodium (DSS)-induced weight loss and diarrhea and impaired colon shortening and potentiated the expression of proinflammatory cytokines and antibacterial peptides in colons of Usp25-/- mice compared to control counterparts. |
References
[1] Wrigley JD, et al. Identification and Characterization of Dual Inhibitors of the USP25/28 Deubiquitinating EnzymeSubfamily. ACS Chem Biol. 2017 Dec 15;12(12):3113-3125. DOI:10.1021/acschembio.7b00334
[2] Xiao-Meng Wang, et al. The deubiquitinase USP25 supports colonic inflammation and bacterial infection and promotes colorectal cancer. Nature Cancer volume 1, pages811–825(2020).
AZ-1 Preparation Products And Raw materials
Raw materials
Preparation Products
AZ-1 Suppliers
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- 13549236410
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- 021-QQ：65489617 15618227136
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- 21-5161 9052
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