Application
LE 135 has been used for in vitro islet treatment.
Biochem/physiol Actions
LE135 is a retinoic acid receptor (RAR) antagonist with selectivity for RARβ (Ki = 220 nM) over RARα (Ki = 1.4 μM).
LE135 is a retinoic acid receptor (RAR) antagonist with selectivity for RARβ (Ki = 220 nM) over RARα (Ki = 1.4 μM). LE135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at 10 μM), but not RARα, RARγ or retinoid X receptor α (RXRα). There is high interest in retinoic acid receptors for cancer and for differentiation studies. LE135 has been shown to inhibit retinoid Am80-induced differentiation of human promyelocytic leukemia HL-60 cells with an IC50 value of 0.2 μM. LE135 has been used to study the role of a retinoic acid receptor-β (RARβ) on the differentiation of mesenchymal stem cells, and was found to inhibit the neuronal differentiation promoting effects of all-trans retinoic acid (ATRA) on mesenchymal stem cells.
Features and Benefits
This compound is featured on the Nuclear Receptors (Non-Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | yellow to orange |
| solubility | DMSO: 15 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | N1(c2c(cc5c(c2)C(CCC5(C)C)(C)C)N=C(c4c1cccc4)c3ccc(cc3)C(=O)O)C |
| InChI | 1S/C29H30N2O2/c1-28(2)14-15-29(3,4)22-17-25-23(16-21(22)28)30-26(18-10-12-19(13-11-18)27(32)33)20-8-6-7-9-24(20)31(25)5/h6-13,16-17H,14-15H2,1-5H3,(H,32,33) |
| InChI key | YZZAIQOVMHVWBS-UHFFFAOYSA-N |
