NU-8165
NU-8165 is an inhibitor of the MDM2-p53 protein-protein interaction with anti-tumor activity. Optimization of NU-8165 was guided by MDM2 NMR titrations, which indicated key binding interaction regions. NU-8165 activated MDM2 and p21 transcription in cell-based assays and showed modest selectivity for wild-type p53 cell lines.
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- No. CAS: 849723-20-2
- Fòrmula: C24H22ClNO3
- Peso molecular:407.89
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | GI50 |
79 μM
Compound: 4a
|
Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay
Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay
|
[PMID: 29089230] |
| HCT-116 | GI50 |
90 μM
Compound: 4a
|
Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay
Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay
|
[PMID: 29089230] |
| SJSA-1 | IC50 |
15.9 μM
Compound: 2c
|
Inhibitory concentration against MDM2-p53 interaction in SJSA human sarcoma cells
Inhibitory concentration against MDM2-p53 interaction in SJSA human sarcoma cells
|
[PMID: 15713419] |
Chemical Information
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No. CAS 849723-20-2
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Peso molecular 407.89
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Fòrmula C24H22ClNO3
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SMILES
O=C1N(CC2=CC=CC=C2)C(OCCCO)(C3=CC=C(Cl)C=C3)C4=C1C=CC=C4
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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)