CSN5-14
CSN5-14 is a CSN5 inhibitor (IC50 0.73 μM). CSN5-14 blocks the removal of NEDD8 from Cullin, leading to the accumulation of NEDD8-Cul1. CSN5-14 induces intracellular ROS accumulation. CSN5-14 induces cell cycle arrest and Apoptosis. CSN5-14 does not induce detectable cellular senescence. CSN5-14 exhibits anticancer activity against triple-negative breast cancer.
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- Formule: C29H33N5O2
- Masse moléculaire:483.60
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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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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
8.1 μM
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Cytotoxicity against human MDA-MB-231 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Cytotoxicity against human MDA-MB-231 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42858571 |
| MDA-MB-468 | IC50 |
5.8 μM
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Cytotoxicity against human MDA-MB-468 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Cytotoxicity against human MDA-MB-468 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42858571 |
| MCF-10A | IC50 |
14.1 μM
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Cytotoxicity against human MCF-10A cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Cytotoxicity against human MCF-10A cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42858571 |
In Vitro
CSN5-14 (0.39-100 μM; 72 h) reduces the viability of MDA-MB-231 and MDA-MB-468 cells, with an IC50 of 8.1 μM in MDA-MB-231 and 5.8 μM in MDA-MB-468[1].
CSN5-14 (5-20 μM; 24 h) dose-dependently inhibits DNA replication in MDA-MB-231 cells, with EdU incorporation decreasing to 34.1% at 5 μM and to below 10% at 10-20 μM[1].
CSN5-14 (5-20 μM; 24 h exposure) impairs the long-term clonogenic survival of MDA-MB-231 and MDA-MB-468 cells, with almost complete inhibition at 20 μM[1].
CSN5-14 (5-20 μM; 24 h) does not induce detectable cellular senescence in MDA-MB-231 cells[1].
CSN5-14 (2.5-5 μM; 0-36 h) does not significantly affect MDA-MB-231 migration[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 and MDA-MB-468 cells
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Concentration:2.5, 5, 10, 20 μM (12 h); 20 μM (0, 2, 4, 8, 12, 24 h)
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Incubation Time:12 h (dose-dependent); 0, 2, 4, 8, 12, 24 h (20 μM time-course)
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Result:NEDD8-Cul1/Cul1 fold change was 1.45 at 2.5 μM, 1.84 at 5 μM, 2.29 at 10 μM, and 2.73 at 20 μM in MDA-MB-231 cells.
The ratios were 1.36, 1.83, 2.17, and 2.48 at 2.5, 5, 10, and 20 μM, respectively, in MDA-MB-468 cells.
NEDD8-Cul1 was detectable by 2 h, sustained through 12 h, and slightly decreased at 24 h.
Total CSN5 protein remained stable across dose groups.
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Cell Line:MDA-MB-231, MDA-MB-468, and MCF-10A cells
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Concentration:0.39-100 μM
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Incubation Time:72 h
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Result:IC50 was 8.1 μM in MDA-MB-231, 5.8 μM in MDA-MB-468, and 14.1 μM in MCF-10A cells.
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Cell Line:MDA-MB-231 cells
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Concentration:5, 10, 20 μM
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Incubation Time:24 h
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Result:The EdU-positive rate was 34.1% at 5 μM and fell below 10% at 10 μM and 20 μM.
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Cell Line:MDA-MB-231 cells
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Concentration:2.5, 5 μM
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Incubation Time:0, 12, 24, 36 h
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Result:No significant changes in migratory potential were detected between exposed and control groups over 36 h.
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Cell Line:MDA-MB-231 cells
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Concentration:2.5, 5, 10, 20 μM
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Incubation Time:24 h
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Result:G0/G1 fractions increased to 45.6%, 49.9%, and 56.8% at 2.5, 5, and 10 μM, respectively, with a concomitant decrease in S-phase cells.
At 20 μM, cells accumulated predominantly in G2/M, with the G2/M fraction reaching 66.9%.
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Cell Line:MDA-MB-468 and MDA-MB-231 cells
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Concentration:5, 10, 20 μM
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Incubation Time:72 h
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Result:In MDA-MB-468 cells, total apoptotic rates were ~27.7% at 10 μM and ~45.6% at 20 μM.
In MDA-MB-231 cells, the total apoptotic rate was ~32.8% at 20 μM.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Senescence-associated β-galactosidase staining
Parmacokinetics
| Species | Dose | Route | Tmax | Cmax | AUC0-24 | AUC0-∞ | T1/2 | CLz/F | Vz/F |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 0.14 h | 2950.76 μg/L | 4105.63 μg/L·h | 4106.12 μg/L·h | 1.81 h | 2.46 L/h/kg | 6.31 L/kg |
Chemical Information
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Masse moléculaire 483.60
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Formule C29H33N5O2
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SMILES
O=C(NCCCNC1=C2C(NC(C3=CC=C(C)C=C3C4=CC=CC=C4)=C2)=NC=C1)CN5CCOCC5
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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)
CSN5-14 Related Classifications
HY-190503 Related Classifications
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