CSN5-IN-3
CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC50 of 0.58 μM. CSN5-IN-3 inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, and upregulates P53 and Cleaved caspase-3. CSN5-IN-3 exhibits anticancer activity against triple-negative breast cancer.
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- Formule: C27H31N5O
- Masse moléculaire:441.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
Caspase 3 |
Bcl-2 |
CSN5 0.58 μM (IC50) |
In Vitro
CSN5-IN-3 (20 min) acts as a potent CSN5 inhibitor in cell-free fluorescence polarization assays, with an IC50 of 0.58 μM[1].
CSN5-IN-3 (72 h) potently inhibits the viability of MDA-MB-231 cells, with an IC50 value of 2.1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 human triple-negative breast cancer cells
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Concentration:2.5-20 μM (direct treatment); 10 μM (following 2 h preincubation with MG132 or MLN4924)
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Incubation Time:12 h
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Result:Dose-dependently increased NEDD8-Cul1 protein levels while not altering CSN5 expression.
Dose-dependently reduced PD-L1 protein levels.
Dose-dependently upregulated P53, and cleaved caspase-3 protein levels.
Dose-dependently downregulated Bcl-2 protein levels.
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Cell Line:MDA-MB-231 human triple-negative breast cancer cells
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Concentration:1-10 μM
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Incubation Time:24 h
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Result:Caused no significant change in G0/G1 phase cell percentage at 1 μM.
Increased G0/G1 phase cell percentage by 9.6% compared to control at 5 μM (p < 0.01).
Increased G0/G1 phase cell percentage by 18.3% compared to control at 10 μM (p < 0.001).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 4 weeks old, triple-negative breast cancer subcutaneous xenograft model)[1]
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Dosage:8 mg/kg; 16 mg/kg
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Administration:i.p.; every 3 days; 21 days
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Result:Achieved 68.3% tumor growth inhibition (TGI) at 8 mg/kg.
Achieved 89.3% tumor growth inhibition (TGI) at 16 mg/kg.
Showed no mortality in either treatment group.
Exhibited no significant body weight changes in the low-dose group; caused a slight temporary body weight decrease but no significant end-of-study weight loss in the high-dose group.
Reduced PD-L1 and Ki67 expression, and increased P21 expression in excised tumors via immunohistochemical analysis.
Chemical Information
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Masse moléculaire 441.57
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Formule C27H31N5O
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SMILES
CC1=CC=C(C(C2=CC(OC)=CC=C2)=C1)C3=CC4=C(N3)N=CC=C4NCCN5CCNCC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CSN5-IN-3 Related Classifications
HY-181795 Related Classifications
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