(E/Z)-DMU2105
(E/Z)-DMU2105 (Compound 7k) is a potent and highly selective CYP1B1 inhibitor. (E/Z)-DMU2105 inhibits human CYP1B1 enzyme bound to yeast-derived microsomes with an IC50 value of 10 nM. (E/Z)-DMU2105 also potently inhibits CYP1B1 expressed within ‘live’ recombinant yeast and human HEK293 kidney cells with an IC50 value of 63.65 nM. (E/Z)-DMU2105 can be used for the research of cancer, glaucoma, ischemia and obesity.
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- CAS. Nr.: 1031063-36-1
- Formel: C18H13NO
- Molecular Weight:259.30
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
IC50: 10 nM (CYP1B1); 63.65 nM (human HEK293 kidney cells)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
1 μM
Compound: 7k; DMU2105
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Inhibition of human CYP1B1 expressed in HEK293 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin EC50 at 0.02 uM by MTT assay (Rvb = 61 +/- 8 uM)
Inhibition of human CYP1B1 expressed in HEK293 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin EC50 at 0.02 uM by MTT assay (Rvb = 61 +/- 8 uM)
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[PMID: 28222316] |
| HEK293 | EC50 |
8.5 μM
Compound: 7k; DMU2105
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Potentiation of cisplatin-induced cytotoxicity against HEK293 cells by measuring cisplatin EC50 at 10 times CYP1B1 inhibitory IC50 by MTT assay (Rvb = 8.7 +/- 0.7 uM)
Potentiation of cisplatin-induced cytotoxicity against HEK293 cells by measuring cisplatin EC50 at 10 times CYP1B1 inhibitory IC50 by MTT assay (Rvb = 8.7 +/- 0.7 uM)
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[PMID: 28222316] |
| HEK293 | IC50 |
0.004 μM
Compound: 7k; DMU2105
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Inhibition of human liver CYP1B1 expressed in HEK293 cells using CEC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
Inhibition of human liver CYP1B1 expressed in HEK293 cells using CEC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
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[PMID: 28222316] |
| HEK293 | IC50 |
0.053 μM
Compound: 7k; DMU2105
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Inhibition of human liver CYP1B1 expressed in HEK293 cells using 7-ethoxyresorufin as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
Inhibition of human liver CYP1B1 expressed in HEK293 cells using 7-ethoxyresorufin as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
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[PMID: 28222316] |
Chemical Information
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CAS. Nr. 1031063-36-1
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Molecular Weight 259.30
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Formel C18H13NO
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SMILES
O=C(C1=CC=CN=C1)/C=C/C2=CC=C3C=CC=CC3=C2
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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)
(E/Z)-DMU2105 Related Classifications
HY-101284A Related Classifications
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