| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
USP28 0.04 μM (IC50)
USP28-IN-4 targets ubiquitin-specific protease 28 (USP28), a deubiquitinating enzyme involved in regulating DNA repair, cell cycle progression, and apoptosis. It inhibits USP28 with an IC50 of 0.04 μM. The compound shows selectivity for USP28 over other deubiquitinases. |
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| ln Vitro |
USP28-IN-4 (compound 9p) (12.5 μM, 15 μM; 3 d), suppresses the development of colonies in human colorectal cancer cells HCT116 (15 μM) and Ls174T (12.5 μM) [1]. By promoting its breakdown via the ubiquitin-proteasome system (UPS), USP28-IN-4 (20-80 μM; 24 hours) reduces the levels of c-Myc [1].
USP28-IN-4 shows cytotoxicity against human colorectal cancer and lung squamous cell carcinoma cells. It downregulates the cellular level of c-Myc through the ubiquitin-proteasome system in a dose-dependent manner. The compound also decreases ankyrase-1/2 levels in vitro. |
| ln Vivo |
In vivo activity data for USP28-IN-4 are limited. As a USP28 inhibitor with anticancer activity, it is expected to have antitumor effects in xenograft models. Further in vivo studies are needed to fully characterize its efficacy and safety profile.
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| Enzyme Assay |
In vitro enzyme assays measure USP28 inhibition using recombinant USP28 enzyme. IC50 values are determined by assessing deubiquitinase activity in the presence of varying concentrations of USP28-IN-4. Selectivity is confirmed by testing against other deubiquitinases.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Human colorectal cancer cells HCT116 and Ls174T Tested Concentrations: 20 μM, 30 μM, 50 μM, and 60 μM, for Ls174T; 30 μM, 50 μM, 60 μM and 80 μM for HCT116 Incubation Duration: 24 h Experimental Results: Dose-dependently down-regulated the cellular level of c-Myc. Cell-based assays use human colorectal cancer and lung squamous cell carcinoma cells to measure cytotoxicity. c-Myc protein levels are assessed by Western blot analysis. Ankyrase-1/2 levels are measured to confirm the mechanism of action. |
| Animal Protocol |
In vivo efficacy is evaluated in xenograft models of USP28-dependent cancers. The compound's ability to inhibit tumor growth through USP28 inhibition and c-Myc downregulation is assessed. Further studies are needed to fully characterize its in vivo antitumor activity.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for USP28-IN-4 are limited. As a small molecule USP28 inhibitor with a molecular weight of 461.36 (C22H18Cl2N2O3S), it may have favorable oral bioavailability. Further pharmacokinetic studies are needed to determine its ADME properties.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for USP28-IN-4 are limited. As a USP28 inhibitor, it may have on-target effects related to DNA repair and cell cycle regulation. Standard laboratory safety precautions should be followed. Further toxicological studies are needed for comprehensive safety assessment.
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| References | |
| Additional Infomation |
USP28-IN-4 is a highly potent USP28 inhibitor with an IC50 of 0.04 μM. It shows selectivity for USP28 over other deubiquitinases. The compound displays cytotoxicity against cancer cells by downregulating c-Myc through the ubiquitin-proteasome system. It is a valuable research tool for studying USP28 biology and has potential therapeutic applications in cancer.
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| Molecular Formula |
C22H18CL2N2O3S
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|---|---|
| Molecular Weight |
461.360922336578
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| Exact Mass |
460.041
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| CAS # |
2931509-15-6
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| PubChem CID |
168355498
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| Appearance |
Light yellow to brown solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
728
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CS(=O)(=O)C1=CC(=C(C=C1)C(=O)NC2=CC(=C(C=C2)Cl)C3=CC4=C(CNC4)C=C3)Cl
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| InChi Key |
FZNJOQKABIINMG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H18Cl2N2O3S/c1-30(28,29)17-5-6-18(21(24)10-17)22(27)26-16-4-7-20(23)19(9-16)13-2-3-14-11-25-12-15(14)8-13/h2-10,25H,11-12H2,1H3,(H,26,27)
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| Chemical Name |
2-chloro-N-[4-chloro-3-(2,3-dihydro-1H-isoindol-5-yl)phenyl]-4-methylsulfonylbenzamide
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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)
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| 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 | 2.1675 mL | 10.8375 mL | 21.6750 mL | |
| 5 mM | 0.4335 mL | 2.1675 mL | 4.3350 mL | |
| 10 mM | 0.2168 mL | 1.0838 mL | 2.1675 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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