For research use only. Not for therapeutic Use.
SID 7969543 is a selective SF-1 (steroidogenic factor 1, NR5A1) inhibitor with an IC50 of 760 nM. SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 of 30 nM. SF-1 is a transcription factor belonging to the nuclear receptor superfamily[1][2].
SID 7969543 shows IC50s of >33,333 nM for RORα, VP-16, respectively[1].
SID 7969543 is assayed for functional activity against HEK 293T cells co-transfected with a plasmid encoding full length SF-1 and a second vector allowing expression of the luciferase gene under control of five tandem repeats of the natural SF-1 response element (SFRE). SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 values of 30 ± 15 nM[1].
| Catalog Number | I010766 |
| CAS Number | 868224-64-0 |
| Synonyms | ethyl 2-[2-[2-(2,3-dihydro-1,4-benzodioxin-6-ylamino)-2-oxoethyl]-1-oxoisoquinolin-5-yl]oxypropanoate |
| Molecular Formula | C24H24N2O7 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H24N2O7/c1-3-30-24(29)15(2)33-19-6-4-5-18-17(19)9-10-26(23(18)28)14-22(27)25-16-7-8-20-21(13-16)32-12-11-31-20/h4-10,13,15H,3,11-12,14H2,1-2H3,(H,25,27) |
| InChIKey | KWMBIIQCLUIHDI-UHFFFAOYSA-N |
| SMILES | CCOC(=O)C(C)OC1=CC=CC2=C1C=CN(C2=O)CC(=O)NC3=CC4=C(C=C3)OCCO4 |
| Reference | [1]. Madoux F, et al. Potent, selective and cell penetrant inhibitors of SF-1 by functional ultra-high-throughput screening. Mol Pharmacol. 2008;73(6):1776-1784. [2]. Roth J, et al. Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds. Bioorg Med Chem Lett. 2008;18(8):2628-2632. |
