| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
USP25/28-IN-2 (compound AZ2) (titration range) effectively inhibited the activity of purified recombinant USP28 enzyme in various fluorescent substrate assays, with IC50 values ranging from 0.9 to 1.3 μM [1]. USP25/28-IN-2 (AZ2) (titration range; 10 μM) effectively inhibited the activity of purified recombinant USP25 enzyme in fluorescent substrate assays, with an IC50 value of 0.88 μM [1]. USP25/28-IN-2 (AZ2) (200 μM) specifically and reversibly bound purified recombinant USP28 protein, and its dissociation constant (Kd) was determined to be 0.9 μM by isothermal titration calorimetry (ITC) [1]. USP25/28-IN-2 (AZ2) (titration range) specifically bound purified recombinant USP28 protein, and its dissociation constant (Kd) was determined to be 10.3 μM by microcalorimetry (MST) [1]. USP25/28-IN-2 (AZ2) (0.01-60 μM; 2 hours) can bind to endogenous USP28 in HCT116 cells, with an EC50 value of 18.2 μM as measured by the Ub-VS probe competition method [1]. USP25/28-IN-2 (AZ2) (0.01-60 μM; 2 hours) can bind to endogenous USP25 in HCT116 cells, with an EC50 value of 11.5 μM as measured by the Ub-VS probe competition method [1]. After 3 hours of treatment with USP25/28-IN-2 (AZ2) (0-100 μM; 3 hours), the level of endogenous total c-Myc protein in HCT116 cells was reduced in a dose-dependent manner [1]. USP25/28-IN-2 (AZ2) (0-100 μM; 3 h) can induce apoptosis in HCT116 cells in a dose-dependent manner, and this effect was detected by PARP lysis 3 hours after treatment [1]. USP25/28-IN-2 (AZ2) (0-100 μM; 72 h) showed dose-dependent antiproliferative effects in a variety of cancer cell lines (including HCT116, HT29 and SW480) and tissue-matched normal cell lines. After 72 hours of treatment, its EC50 value in cancer cells was approximately 20 μM and its EC50 value in normal cells was approximately 28 μM [1].
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|---|---|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: HCT116 colon cancer cells Tested Concentrations: 0-100 μM Incubation Duration: 3 hours Experimental Results: Endogenous total c-Myc protein levels decreased in a dose-dependent manner, with complete reduction observed at the highest test concentration. USP28 protein levels remained unchanged (confirming no widespread protein degradation). Apoptosis analysis [1] Cell Types: HCT116 colon cancer cells Tested Concentrations: 0-100 μM Incubation Duration: 3 hours Experimental Results: PARP lysis was induced in a dose-dependent manner, with the most significant lysis occurring after complete downregulation of c-Myc. No PARP lysis was observed at lower concentrations where c-Myc levels were not completely reduced. Cell viability assay [1] Cell Types: HCT116 colon cancer cells, HT29 colorectal adenocarcinoma cells, SW480 colorectal adenocarcinoma cells, 21 cancer cell lines, and 7 tissue-matched normal cell lines Tested Concentrations: 0-100 μM (incrementing in 1/2 log units) Incubation Duration: 72 hours Experimental Results: In HCT116 cells, cell viability decreased in the EC50 range of 18.0-20.0 μM. Similar dose-dependent antiproliferative activity was observed in HT29 and SW480 cells. In all 21 cancer cell lines, cell viability decreased, with EC50 values concentrated around 20 μM. In the 7 normal cell lines, cell viability decreased, with EC50 values concentrated around 28 μM, indicating a small therapeutic window. |
| References |
| Molecular Formula |
C17H17BRF3NO3
|
|---|---|
| Molecular Weight |
420.23
|
| CAS # |
2165322-95-0
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC(F)(F)OC1=CC=CC(=C1)COC2=CC=C(Br)C=C2CNCCO
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3796 mL | 11.8982 mL | 23.7965 mL | |
| 5 mM | 0.4759 mL | 2.3796 mL | 4.7593 mL | |
| 10 mM | 0.2380 mL | 1.1898 mL | 2.3796 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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