CAS-010
CAS-010 (CAS-13312-010) is a potent and selective USP28 inhibitor with an IC50 of 2.2 nM against full-length USP28. CAS-010 acts as a ubiquitin-competitive inhibitor and shows higher selectivity over USP25 (IC50 = 51 nM) and other USP family members, disrupting the 53BP1-USP28 interaction and suppressing p53-dependent transcription of CDKN1A (p21), MDM2, and BAX. CAS-010 can be used for studying USP28-mediated DNA damage response and p53 signaling in cancer-related research.
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- No. CAS: 3094094-17-1
- Fòrmula: C26H32N4OS
- Peso molecular:448.62
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
USP28 2.2 nM (IC50) |
USP25 51 nM (IC50) |
In Vitro
CAS-010 (0.1-10 μM; 24 h) regulates the p53 transcriptional program, upregulates p21 and MDM2 expression, and promotes 53BP1-USP28 complex formation in U2OS cells[1].
CAS-010 (0.03-10 μM; 24 h) induces p53 target gene expression and enhances p53 transcriptional activity in HCT116 cells[1].
CAS-010 (dose-dependent; 5 d) inhibits the proliferation of multiple cancer cell lines, and its cellular activity profile strongly correlates with the USP28 knockout phenotype[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:U2OS cells
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Concentration:5 μM
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Incubation Time:24 h + Nutlin-3a (4 h)
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Result:Reduced CDKN1A, MDM2 and BAX mRNA expression.
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Cell Line:RPE-1 cells
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Concentration:5 μM
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Incubation Time:24 h + Nutlin-3a (4 h)
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Result:Suppressed p53 target gene induction including CDKN1A, MDM2 and BAX.
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Cell Line:Multiple TP53 wild-type cell lines
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Concentration:0.1-10 μM
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Incubation Time:24 h
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Result:Decreased p21 protein levels in a dose-dependent manner across all TP53 wild-type cell lines examined.
Did not alter c-Myc protein abundance under the same conditions.
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Cell Line:CALU-1 cell lines
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Concentration:0.1-10 μM
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Incubation Time:24 h
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Result:Failed to affect p21 protein expression in TP53-null CALU-1 cells.
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Cell Line:RPE-1 cell lines
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Concentration:0.1-10 μM, with or without ionizing radiation
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Incubation Time:24 h
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Result:Reduced p21 and p53 protein levels irrespective of IR exposure.
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Cell Line:~800 cancer cell lines
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Concentration:14 nM-30 μM
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Incubation Time:5 days
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Result:Induced dose-dependent reduction in cell viability, with strongest correlation to USP28 and TP53 pathway dependency signatures.
Parmacokinetics
Chemical Information
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No. CAS 3094094-17-1
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Peso molecular 448.62
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Fòrmula C26H32N4OS
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SMILES
O=C(C1=C(N)C2=C(N=C(CCC)C=C2)S1)NCCC3=CC=C(C4CC5NC(C4)CC5)C=C3
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Synonyms
CAS-13312-010
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CAS-010 Related Classifications
HY-184244 Related Classifications
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