BMS-189453
Biochem/physiol Actions
BMS-189453 specifically has sufficient bioavailability in rats and monkeys. BMS-189453 only binds to ?, ?, and ? retinoid receptors but its activation is unknown. BMS-189453 is found to inhibit the action of collagenase-3 (MMP-13) which catalyses cartilage matrix degradation. Thus, it serves to treat rheumatoid arthritis.
BMS-189453 is a potent RARβ agonist that acts as an antagonist against RARα and RARγ. BMS-189453 induces RARβ reporter gene expression at sub nanomolar levels, and is 30 fold more potent than all-trans retinoic acid for inducing TGFβ activity in normal breast cells. The compound BMS-189453 does not transactivate RARα or γ transcriptional activity, but binding to those family members induces a strong transrepression of phorbol ester-induced AP-1 activity (IC50 = 0.1 nM in HeLa and MCSF-7). BMS-189453 significantly increases the efficiency of cardiac differentiation of hESCs.
Features and Benefits
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
Packaging
5, 25 mg in glass bottle
| Colour | white to beige |
|---|---|
| Quality Level | 100 |
| InChI key | VUODRPPTYLBGFM-CMDGGOBGSA-N |
| InChI | 1S/C27H24O2/c1-27(2)17-16-23(21-6-4-3-5-7-21)24-18-20(12-15-25(24)27)9-8-19-10-13-22(14-11-19)26(28)29/h3-16,18H,17H2,1-2H3,(H,28,29)/b9-8+ |
| Manufacturer | SIGMA-ALDRICH |
| Solubility | DMSO: 10 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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