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
- Molecular Weight:
- 422.21
- MDL Number:
- MFCD32201047
- MOL File:
- 2165322-94-9.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| 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 |
| UNSPSC Code | 12352200 |
| NACRES | NA.21 |
AZ-1 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 40335 | AZ1 USP25/28 Inhibitor ≥98% | 2165322-94-9 | 5mg | $83 | 2026-04-30 | Buy |
| Cayman Chemical | 40335 | AZ1 USP25/28 Inhibitor ≥98% | 2165322-94-9 | 10mg | $132 | 2026-04-30 | Buy |
| Cayman Chemical | 40335 | AZ1 USP25/28 Inhibitor ≥98% | 2165322-94-9 | 25mg | $269 | 2026-04-30 | Buy |
| Cayman Chemical | 40335 | AZ1 USP25/28 Inhibitor ≥98% | 2165322-94-9 | 50mg | $413 | 2026-04-30 | Buy |
| ChemScene | CS-0065552 | USP25/28 inhibitor AZ1 98.0% | 2165322-94-9 | 5mg | $87 | 2026-06-04 | Buy |
AZ-1 Chemical Properties, Uses, 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; 40mg/kg; gavage; daily; for 7days) protects from dextran sulfate sodium (DSS)-induced weight loss and diarrhea and impaired colon shortening[1].
USP25/28 inhibitor AZ1 (20mg/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 (20mg/kg/day; gavage; every 3days 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: | 40mg/kg |
| Administration: | Gavage; daily; for 7days |
| 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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| InvivoChem | 13549236410 | sales@invivochem.cn | China | 6745 | 58 |
| Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7717 | 56 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4859 | 55 | |
| Shanghai Beckham Medical Technology Co., Ltd | 13816613772 | huahero21@sina.com | China | 2994 | 55 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| ShangHai Biochempartner Co.,Ltd | 177-54423994 17754423994 | 2853530910@QQ.com | China | 8000 | 62 |
| Shanghai Chaolan Chemical Technology Center | QQ：65489617 13301690235 | Sales@ATKchemical.com | China | 9729 | 58 |
| Beijing Solarbio Science & Tecnology Co., Ltd. | 17801761073 18101056239 | 3193328036@qq.com | China | 28150 | 68 |
| Chuzhou KeMail Chemical Technology Co., Ltd | 0550-5196001 15000891977 | wj520wjxby@126.com | China | 1940 | 55 |
| Shanghai Tube Pharmaceutical Co., Ltd. | 021-54338626 18017892860 | sales@tubepharm.com | China | 2709 | 58 |
