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TMS
- Trans-2,3',4,5'-tetramethoxystilbene
- Soluble in DMSO
- MF: C18H20O4
- MW: 300.35
Description
TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a highly potent, selective and competitive inhibitor of CYP1B1 enzyme. It demonstrates clear isoform selectivity with IC50 values of 6 nM (CYP1B1), 300 nM (CYP1A1), and 3100 nM (CYP1A2). TMS enhances the inhibition of cell growth and drives apoptosis across various human cancer cells. TMS is widely utilized to characterize CYP1B1 enzyme properties and investigate its pathophysiological role in hypertension.
CYP1B1 pharmacology is relevant to cancer, hypertension; TMS supports mechanistic studies of CYP1B1, apoptosis in biochemical, cellular and disease-model assays.
Key Features
- Highly potent CYP1B1 inhibitor with IC50 of 6 nM
- Targets CYP1B1 without disturbing similar CYP1A1/CYP1A2 enzymes
- Triggers self-destruction in drug-resistant breast cancer cells
- Supports focused CYP1B1 pathway studies in biochemical and cellular systems
Applications
- CYP1B1 pharmacology and target-validation studies
- Oncology research and CYP1B1-mediated downstream signaling pathways studies
- Disease-model research related to cancer, hypertension
- Compound profiling, assay development and lead-optimization support
More Information
| Parent CAS No. | 24144-92-1 |
|---|---|
| Chemical Name | (E)-4,5'-(ethene-1,2-diyl)bis(1,3-dimethoxybenzene) |
| SMILES | C1(/C=C/C2=CC(OC)=CC(OC)=C2)=CC=C(OC)C=C1OC |
| MFCD | MFCD03428621 |
| InChi | InChI=1S/C18H20O4/c1-19-15-8-7-14(18(12-15)22-4)6-5-13-9-16(20-2)11-17(10-13)21-3/h5-12H,1-4H3/b6-5+ |
| InChiKey | JDBCWSHYEQUBLW-AATRIKPKSA-N |
| CID | 5354004 |
| Short Description | CYP1B1 inhibitor |
References
- S Kim et al. Design, synthesis, and discovery of novel trans-stilbene analogues as potent and selective human cytochrome P450 1B1 inhibitors. J Med Chem. 2002 Jan 3;45(1):160-4.
- KA Nam et al. Resveratrol analog, 3,5,2',4'-tetramethoxy-trans-stilbene, potentiates the inhibition of cell growth and induces apoptosis in human cancer cells. Arch Pharm Res. 2001 Oct;24(5):441-5.
- KU Malik et al. Contribution of cytochrome P450 1B1 to hypertension and associated pathophysiology: a novel target for antihypertensive agents. Prostaglandins Other Lipid Mediat. 2012 Aug;98(3-4):69-74.
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