DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively. DMU2139 showed a very high level of selectivity towards CYP1B1 with respect to the IC50 values obtained with CYP1A1, CYP1A2, CYP3A4, CYP2D6, CYP2C9 and CYP2C19 Sacchrosomes™.
CAS Number: 1821143-80-9
Molecular Weight: 289.33
Chemical Name: (E)-1-(6-methoxynaphthalen-2-yl)-3-(pyridin-3-yl)prop-2-en-1-one
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
DMU2139 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.
- Horley NJ, Beresford KJ, Chawla T, McCann GJ, Ruparelia KC, Gatchie L, Sonawane VR, Williams IS, Tan HL, Joshi P, Bharate SS, Kumar V, Bharate SB, Chaudhuri B. 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. doi: 10.1016/j.ejmech.2017.02.016. Epub 2017 Feb 9. PMID: 28222316.
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