1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. (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.

For research use only. We do not sell to patients.

(E/Z)-DMU2105

(E/Z)-DMU2105 Chemical Structure

CAS No. : 1031063-36-1

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Description

(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[1].

IC50 & Target

IC50: 10 nM (CYP1B1); 63.65 nM (human HEK293 kidney cells)[1]

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
1 μM
Compound: 7k; DMU2105
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)
[PMID: 28222316]
HEK293 EC50
8.5 μM
Compound: 7k; DMU2105
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)
[PMID: 28222316]
HEK293 IC50
0.004 μM
Compound: 7k; DMU2105
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
[PMID: 28222316]
HEK293 IC50
0.053 μM
Compound: 7k; DMU2105
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
[PMID: 28222316]
Molecular Weight

259.30

Formula

C18H13NO

CAS No.
SMILES

O=C(C1=CC=CN=C1)/C=C/C2=CC=C3C=CC=CC3=C2

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
(E/Z)-DMU2105
Cat. No.:
HY-101284A
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