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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- CAS 番号: 3094094-17-1
- 分子式: C26H32N4OS
- 分子量:448.62
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保管条件:
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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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
USP28 2.2 nM (IC50) |
USP25 51 nM (IC50) |
体外実験
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
化学情報
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CAS 番号 3094094-17-1
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分子量 448.62
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分子式 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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別名
CAS-13312-010
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CAS-010 関連分類
HY-184244 関連分類
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