T-10531
T-10531 is a selective USP25/USP28 inhibitor. T-10531 exhibits an IC50 of 0.03 μM and a Kd of 0.2 μM against human USP25, as well as an IC50 of 0.12 μM and a Kd of 0.06 μM against human USP28. T-10531 inhibits USP25/USP28 activity and induces the degradation of USP25 via the proteasomal pathway, without inhibiting other deubiquitinases. T-10531 can be used in the research of squamous cell carcinoma, colorectal cancer, gastric cancer, triple-negative breast cancer and pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 3129176-25-3
- Formula: C26H22BrClF4N2O5S
- Molecular Weight:665.88
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
T-10531 (compound 42) potently inhibits recombinant USP25 with an IC50 of 0.03 μM and recombinant USP28 with an IC50 of 0.12 μM in a Ub-Rho110 cleavage assay[1].
T-10531 binds to recombinant USP25 with a Kd of 0.2 μM and to recombinant USP28 with a Kd of 0.06 μM in an ITC assay[1].
T-10531 (72 h) exhibits no toxicity to HepG2 hepatocellular carcinoma cells[1].
T-10531 directly binds and stabilizes recombinant USP25, causing a 7.0 °C thermal shift, and recombinant USP28, causing a 3.8 °C thermal shift in a DSF assay[1].
T-10531 (0.1-50 μM; 4 h, 10 μM; 10-240 min) dose-dependently inhibits USP25 and USP28 activity in live HeLa cells without affecting other DUBs, and induces proteasome-dependent degradation of USP25 in a time- and dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HeLa cells
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Concentration:0.1, 0.5, 1, 5, 10, 50 μM
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Incubation Time:4 h
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Result:Dose-dependently reduced USP25 protein level and USP25/USP28 activity-based probe labeling.
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Cell Line:HeLa cells
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Concentration:10 μM
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Incubation Time:10, 30, 60, 90, 120, 240 min
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Result:Reduced USP25 protein level in a time-dependent manner.
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Cell Line:HeLa cells
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Concentration:0.1, 0.5, 1, 5, 10 μM (with 750 nM MG132 (HY-13259))
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Incubation Time:4 h
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Result:Reduced USP25 protein level, which is rescued by the proteasome inhibitor MG132.
Reduced USP25 protein level regardless of USP28 knockdown.
Chemical Information
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CAS No. 3129176-25-3
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Molecular Weight 665.88
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Formula C26H22BrClF4N2O5S
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SMILES
O=C(NC1=CC(F)=C(F)C(COC2=CC(F)=C(Br)C=C2CN3C[C@@H](O)CC3)=C1F)C4=CC=C(S(=O)(C)=O)C=C4Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
T-10531 Related Classifications
HY-183604 Related Classifications
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