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.
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- CAS. Nr.: 3129176-25-3
- Formel: C26H22BrClF4N2O5S
- Molecular Weight:665.88
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
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.
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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. Nr. 3129176-25-3
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Molecular Weight 665.88
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
T-10531 Related Classifications
HY-183604 Related Classifications
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