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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- CAS. Nr.: 849723-20-2
- Formel: C24H22ClNO3
- Molecular Weight:407.89
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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Cell Line
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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
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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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CAS. Nr. 849723-20-2
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Molecular Weight 407.89
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)