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.
For research use only. We do not sell to patients.
- CAS No.: 3094094-17-1
- Formula: C26H32N4OS
- Molecular Weight:448.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
|
USP28 2.2 nM (IC50) |
USP25 51 nM (IC50) |
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.
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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.
Chemical Information
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CAS No. 3094094-17-1
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Molecular Weight 448.62
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Formula 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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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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