ChemicalBook > CAS DataBase List > AZ-1

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

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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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0065552
Product name: USP25/28inhibitorAZ1
Purity: 98.10%
Packaging: 5mg
Price: $150
Updated: 2021/12/16

ChemScene

Product number: CS-0065552
Product name: USP25/28inhibitorAZ1
Purity: 98.10%
Packaging: 10mg
Price: $250
Updated: 2021/12/16

ChemScene

Product number: CS-0065552
Product name: USP25/28inhibitorAZ1
Purity: 98.10%
Packaging: 25mg
Price: $500
Updated: 2021/12/16

ChemScene

Product number: CS-0065552
Product name: USP25/28inhibitorAZ1
Purity: 98.10%
Packaging: 50mg
Price: $850
Updated: 2021/12/16

ChemScene

Product number: CS-0065552
Product name: USP25/28inhibitorAZ1
Purity: 98.10%
Packaging: 100mg
Price: $1450
Updated: 2021/12/16

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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;Trp53^fl/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

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2165322-94-9, AZ-1Related Search:

USP25 and 28 inhibitor AZ-1

Ethanol, 2-[[[5-bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]-

AZ-1;AZ 1;AZ1

USP25/28 inhibitor AZ1

2-((5-bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)benzyl)amino)ethanol

AZ-1

Deubiquitinase,USP-25/28 inhibitor AZ1,USP25/28 inhibitor AZ1,inhibit,AZ 1,Inhibitor,AZ-1,DUBs

2-((5-Bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)benzyl)amino)ethan-1-ol

AZ1 USP25/28 inhibitor

USP25/28 inhibitor AZ1, 10 mM in DMSO

2165322-94-9

C17H16BrF4NO2