DMU2139(CYP1B1 inhibitor 6j)

Modify Date: 2024-01-16 08:26:53

DMU2139(CYP1B1 inhibitor 6j) Structure
DMU2139(CYP1B1 inhibitor 6j) structure
Common Name DMU2139(CYP1B1 inhibitor 6j)
CAS Number 1821143-80-9 Molecular Weight 289.33
Density N/A Boiling Point N/A
Molecular Formula C19H15NO2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of DMU2139(CYP1B1 inhibitor 6j)


DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.

 Names

Name DMU2139

 DMU2139(CYP1B1 inhibitor 6j) Biological Activity

Description DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
Related Catalog
Target

CYP1B1:9 nM (IC50)

CYP1A1:795 nM (IC50)

In Vitro DMU2139 (6j) shows 88 and 133-fold selectivity for CYP1B1 over CYP1A1 and CYP1A2. In the presence of DMU2139, the EC50 is reversed back to 8.3 μM from 61 μM (seen in CYP1B1-expressing cells without any inhibitor). The EC50 value, in the presence of DMU2139, resembles the EC50 of cisplatin, 8.7μM, in cells transfected with the empty plasmid which has no CYP1B1 gene and therefore cannot express CYP1B1 protein[1].
References

[1]. Horley NJ, et al. Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines. Eur J Med Chem. 2017 Mar 31;129:159-174.

 Chemical & Physical Properties

Molecular Formula C19H15NO2
Molecular Weight 289.33
Storage condition 2-8℃