| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Ubiquitin-specific protease 7 (USP7) and ubiquitin-specific protease 47 (USP47).
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|---|---|
| ln Vitro |
USP7/USP47 inhibitor (compound 14) has an EC50 of 0.42 μM and 1 μM, respectively, making it a selective inhibitor of USP7/USP47. The 20S proteasome, caspase 3, calpain 1, and a representative panel of USPs (USP2, USP5, USP8, USP21, and USP28; EC50 > 31.6 μM) were not inhibited by USP7/USP47 inhibitors. HCT-116 cell growth is inhibited by USP7/USP47 inhibitor, with an EC50 of 7.6 μM [1].
INVIVO25371 inhibits USP7 and USP47 with EC50 values of 0.42 μM and 1.0 μM, respectively. By inhibiting these deubiquitinating enzymes, it disrupts the deubiquitination of target proteins, leading to their degradation via the proteasome. Detailed substrate specificity and cellular activity data are available in primary publications. |
| ln Vivo |
INVIVO25371 exhibits anticancer activity by inhibiting USP7 and USP47, leading to the destabilization of oncogenic proteins and induction of cancer cell death. USP7 inhibition is known to destabilize MDM2, leading to p53 activation and apoptosis in p53-wild-type cancers. The compound is used to study the role of USP7/USP47 in cancer biology.
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| Enzyme Assay |
USP7 and USP47 enzymatic activity is measured using deubiquitination assays. Recombinant USP7 or USP47 is incubated with ubiquitin-AMC (a fluorogenic substrate) or polyubiquitinated substrates and varying concentrations of INVIVO25371. The release of free ubiquitin or AMC fluorescence is monitored to determine EC50 values.
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| Cell Assay |
Cancer cell lines sensitive to USP7/USP47 inhibition are treated with INVIVO25371 at various concentrations. Cell viability is assessed by MTT or CellTiter-Glo assays. Ubiquitination and degradation of target proteins (e.g., MDM2, p53) are evaluated by Western blot. Apoptosis is assessed by caspase activation and Annexin V staining.
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| Animal Protocol |
INVIVO25371 is typically evaluated in mouse xenograft models of USP7/USP47-dependent tumors. Tumor-bearing mice are treated with INVIVO25371 via intraperitoneal or oral administration. Tumor growth inhibition, target engagement (ubiquitination changes), and survival are monitored.
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| ADME/Pharmacokinetics |
INVIVO25371 has molecular weight 484.40 and formula C18H11Cl2N3O3S3. It is a solid powder with ≥98% purity. As a small-molecule USP7/USP47 inhibitor, it is suitable for both in vitro and in vivo applications. Detailed PK parameters are available in primary research publications.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for INVIVO25371 are limited. As a USP7/USP47 inhibitor, potential on-target toxicities may include effects on normal cellular processes regulated by these deubiquitinating enzymes.
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| References | |
| Additional Infomation |
INVIVO25371 is a research tool for studying ubiquitin-proteasome pathways and the role of USP7/USP47 in cancer. Its mechanism involves inhibition of USP7 and USP47 deubiquitinase activity, leading to destabilization of oncogenic proteins and induction of apoptosis. No clinical trials or approved indications exist.
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| Molecular Formula |
C18H11CL2N3O3S3
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|---|---|
| Molecular Weight |
484.384
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| Exact Mass |
482.934
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| CAS # |
1247825-37-1
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| PubChem CID |
51031028
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| Appearance |
White to off-white solid powder
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| LogP |
6.593
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
736
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CS(=O)(=O)C1=CC=C(C=C1)NC(=O)C2=CC(=C(S2)SC3=C(C=NC=C3Cl)Cl)C#N
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| InChi Key |
GUDJFFQZIISQJB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H11Cl2N3O3S3/c1-29(25,26)12-4-2-11(3-5-12)23-17(24)15-6-10(7-21)18(27-15)28-16-13(19)8-22-9-14(16)20/h2-6,8-9H,1H3,(H,23,24)
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| Chemical Name |
4-cyano-5-(3,5-dichloropyridin-4-yl)sulfanyl-N-(4-methylsulfonylphenyl)thiophene-2-carboxamide
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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) |
DMSO : ~50 mg/mL (~103.22 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0645 mL | 10.3225 mL | 20.6449 mL | |
| 5 mM | 0.4129 mL | 2.0645 mL | 4.1290 mL | |
| 10 mM | 0.2064 mL | 1.0322 mL | 2.0645 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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