USP7-IN-20
USP7-IN-20 is a highly selective USP7 inhibitor that binds allosterically to the allosteric pocket of USP7 in a non-competitive and reversible manner. USP7-IN-20 downregulates MDM2 protein levels and stabilizes p53, thereby inducing p21 expression and enhancing the ubiquitin-dependent degradation of MDM2. USP7-IN-20 effectively binds endogenous USP7 to inhibit cancer cell proliferation, and also induces apoptosis by promoting the cleavage of PARP and caspase 3. USP7-IN-20 can be widely used in cancer-related basic and translational research.
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- CAS No.: 2196246-28-1
- Formule: C22H24BrN3O3S
- Masse moléculaire:490.41
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
USP7 |
In Vitro
USP7-IN-20 (Compound 2) (0.3 μM; 30 min pre-incubation, 90 min assay) potently inhibits full-length USP7 enzyme activity in vitro with an IC50 of 0.3 μM and binds reversibly to the USP7 catalytic domain with a Kd of 2.6 μM[1].
USP7-IN-20 (0.85 μM; 2 h) potently engages endogenous USP7 in HCT116 colorectal cancer cells with an EC50 of 0.85 μM[1].
USP7-IN-20 (2.6 μM; 24 h) induces MDM2 ubiquitination in SJSA-1 osteosarcoma cells with an EC50 of 2.6 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 colorectal cancer cells
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Concentration:0.85 μM
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Incubation Time:2 h
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Result:Competed with the Ub-PA probe for binding to endogenous USP7 in HCT116 cells with an EC50 of 0.85 μM.
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 2196246-28-1
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Masse moléculaire 490.41
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Formule C22H24BrN3O3S
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SMILES
O=C1C2=C(C(Br)=CS2)N=CN1CC3(CCN(CC3)C(C[C@H](C4=CC=CC=C4)C)=O)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
USP7-IN-20 Related Classifications
HY-183942 Related Classifications
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