1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. (E/Z)-DMU2139

(E/Z)-DMU2139 (Compound 180) is the E/Z isomer of DMU2139 (HY-101285). (E/Z)-DMU2139 is a potent and specific CYP1B1 inhibitor (IC50: 4 nM).

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(E/Z)-DMU2139 Chemical Structure

(E/Z)-DMU2139 Chemical Structure

CAS No. : 104890-70-2

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Description

(E/Z)-DMU2139 (Compound 180) is the E/Z isomer of DMU2139 (HY-101285). (E/Z)-DMU2139 is a potent and specific CYP1B1 inhibitor (IC50: 4 nM)[1].

IC50 & Target

IC50: 4 nM (CYP1B1)[1]

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.004 μM
Compound: 6j; DMU2139
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
0.008 μM
Compound: 6j; DMU2139
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]
HEK293 EC50
8.3 μM
Compound: 6j; DMU2139
Inhibition of human CYP1B1 expressed in HEK293 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin EC50 at 0.018 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 0.018 uM by MTT assay (Rvb = 61 +/- 8 uM)
[PMID: 28222316]
Molecular Weight

289.33

Formula

C19H15NO2

CAS No.
SMILES

O=C(C1=CC=C2C=C(OC)C=CC2=C1)/C=C/C3=CC=CN=C3

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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)-DMU2139
Cat. No.:
HY-126308
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