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USP25/28 inhibitor AZ1 is a selective, orally active and non-competitive dual ubiquitin-specific protease USP25/28 inhibitor with IC50 of 0.7 μM and 0.6 μM, respectively, and exhibits anti-inflammatory and anti-tumor effects.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $30 | In Stock | |
5 mg | $64 | In Stock | |
10 mg | $98 | In Stock | |
25 mg | $222 | In Stock | |
50 mg | $338 | In Stock | |
100 mg | $497 | In Stock | |
500 mg | $1,090 | In Stock | |
1 mL x 10 mM (in DMSO) | $71 | In Stock |
Description | USP25/28 inhibitor AZ1 is a selective, orally active and non-competitive dual ubiquitin-specific protease USP25/28 inhibitor with IC50 of 0.7 μM and 0.6 μM, respectively, and exhibits anti-inflammatory and anti-tumor effects. |
Targets&IC50 | USP28:0.6 nM, USP25:0.7 nM |
In vitro | METHODS: HCT116 cells were treated with USP25/28 inhibitor AZ1 (20, 40, 60, 80, 100 μM) and samples were collected 3 hours later for Western blot analysis of USP28, c-Myc and PARP. RESULTS Western blot analysis showed that the total protein level of c-Myc decreased rapidly and concentration-dependently after treatment with USP25/28 inhibitor AZ1. [1] |
In vivo | Method: USP25/28 inhibitor AZ1 (AZ1) (20, 40mg/kg, gavage) was given to WT Model mice were used to study the effect of USP25/28 inhibitor AZ1 (AZ1) on DSS-induced colitis. RESULTS USP25/28 inhibitor AZ1 (AZ1) treatment significantly reduced the number of colon tumors; the expression of wnt-related genes and pSTAT3 levels in tumors in the USP25/28 inhibitor AZ1 (AZ1) treatment group were reduced, and the SOCS3 level was increased; USP25/28 inhibitor Inflammation and bacterial replication were impaired in the colon of mice gavaged with AZ1 (AZ1), the expression of pro-inflammatory cytokines and antimicrobial peptides was enhanced, p-p65 and p-p38 levels were increased, and TRAF3 levels were decreased. [2] |
Alias | AZ1 |
Molecular Weight | 422.21 |
Formula | C17H16BrF4NO2 |
Cas No. | 2165322-94-9 |
Smiles | OCCNCc1cc(Br)ccc1OCc1ccc(F)c(c1)C(F)(F)F |
Relative Density. | 1.488 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 250 mg/mL (592.12 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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