NEP48
NEP48 is a small-molecule antagonist targeting the ZER1 (E3 ubiquitin ligase)-E7 oncogenic axis. NEP48 binds to the MHGD/N-degron binding pocket within the ARM repeat domain of ZER1, competitively blocking E7-ZER1 binding and ZER1-mediated substrate degradation. NEP48 disrupts the ZER1-E7 interaction, leading to Rb stabilization and silencing of E2F-driven transcriptional programs. NEP48 inhibits the proliferation of HPV-positive cancer cells and can be used for research on HPV-positive cervical cancer.
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- No. CAS: 3108114-67-3
- Fòrmula: C14H16N4O3
- Peso molecular:288.30
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
23.05 μM
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Inhibition of proliferation of ZER1 wild-type HeLa cells assessed as reduction in viable cell count after 4 days of treatment by hemocytometer counting with dose-response curve fitting using non-linear regression analysis.
Inhibition of proliferation of ZER1 wild-type HeLa cells assessed as reduction in viable cell count after 4 days of treatment by hemocytometer counting with dose-response curve fitting using non-linear regression analysis.
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42519832 |
In Vitro
NEP48 (Compound 4) (0.5-200 μM; 4 days) selectively inhibits proliferation of ZER1 wild-type HeLa cells (IC50=23.05 μM) but not ZER1 knockout HeLa or HPV-negative C33A cells[1].
NEP48 (40 μM; 48 h) selectively downregulates E2F target gene expression in HPV-positive HeLa cells but not in HPV-negative C33A cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa (ZER1 wild-type and ZER1 knockout), C33A
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Concentration:0.5-200 μM
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Incubation Time:4 days
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Result:Inhibited HeLa cell growth with an IC50 of 23.05 μM, but this sensitivity was largely abolished in ZER1 knockout HeLa cells.
Had minimal effects on the proliferation of HPV-negative C33A cells.
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Cell Line:HeLa, C33A
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Concentration:40 μM
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Incubation Time:48 h
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Result:Showed top downregulated pathways including MYC targets, G2M checkpoint, E2F targets, and mitotic spindle.
GSEA analyses confirmed marked downregulation of E2F target genes specifically in HeLa cells but not in C33A cells.
RT-qPCR showed consistent downregulation of several representative E2F target genes in HeLa cells, while these genes were paradoxically upregulated in C33A cells.
In Vivo
NEP48 (100-200 mg/kg; i.p.; every other day; 2 weeks) does not inhibit tumor growth in an HPV-negative C33A xenograft model[1].
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 mice (female, 6 weeks old)[1]
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Dosage:100 mg/kg; 200 mg/kg
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Administration:i.p.; every other day; 2 weeks
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Result:Led to significant reductions in tumor volume and weight in HeLa xenografts.
Was well tolerated, with no appreciable weight loss.\nShowed no inhibitory effect on tumor growth in C33A xenografts.
Was well tolerated, with no appreciable weight loss.
Chemical Information
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No. CAS 3108114-67-3
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Peso molecular 288.30
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Fòrmula C14H16N4O3
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SMILES
N[C@H](C(NC1=CC=CN(C1=O)CC2=CC=CC=N2)=O)CO
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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.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NEP48 Related Classifications
HY-189230 Related Classifications
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