Description
(E)-DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
Product information
CAS Number: 1821143-79-6
Molecular Weight: 259.30
Formula: C18H13NO
Chemical Name: (2E)-3-(naphthalen-2-yl)-1-(pyridin-3-yl)prop-2-en-1-one
Smiles: O=C(/C=C/C1=CC2=CC=CC=C2C=C1)C1=CN=CC=C1
InChiKey: VWBDGXJRQZDLRV-CSKARUKUSA-N
InChi: InChI=1S/C18H13NO/c20-18(17-6-3-11-19-13-17)10-8-14-7-9-15-4-1-2-5-16(15)12-14/h1-13H/b10-8+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 33.33 mg/mL (128.54 mM; ultrasonic and warming and heat to 60°C).
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
In Vitro:
(E)-DMU2105 (Compound 7k) shows 74 and 120-fold selectivity for CYP1B1 over CYP1A1 and CYP1A2. In the presence of (E)-DMU2105 however, the EC50 goes down to 1 μM indicating that the cells have suffered from toxicity which may have been mediated by CYP1B1 inhibition. Un-transfected cells (HEK293: pcDNA3.1), when treated with cisplatin and (E)-DMU2105 (10×IC50) do not show any perceptible decrease of cisplatin EC50 (8.5 μM ± 0.9).
References:
- 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.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.