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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.

For research use only. We do not sell to patients.

CAS No.: 2196246-28-1
Formula: C₂₂H₂₄BrN₃O₃S
Molecular Weight:490.41

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

USP7-IN-20 Chemical Structure

CAS No.: 2196246-28-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

USP7

All Deubiquitinase Isoforms :

All PARP Isoforms :

All Caspase Isoforms :

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 K_d 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.

Western Blot Analysis^[1]

Cell Line:

HCT116 colorectal cancer cells
Concentration:

0.85 μM
Incubation Time:

2 h
Result:

Competed with the Ub-PA probe for binding to endogenous USP7 in HCT116 cells with an EC₅₀ of 0.85 μM.

Chemical Information

CAS No. 2196246-28-1
Molecular Weight 490.41
Formula C₂₂H₂₄BrN₃O₃S
SMILES

O=C1C2=C(C(Br)=CS2)N=CN1CC3(CCN(CC3)C(C[C@H](C4=CC=CC=C4)C)=O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Gavory G, et al. Discovery and characterization of highly potent and selective allosteric USP7 inhibitors. Nat Chem Biol. 2018;14(2):118-125. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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USP7-IN-20

All Deubiquitinase Isoforms

All PARP Isoforms

All Caspase Isoforms