Bioactivity | 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]. | ||||||||||||
Invitro | 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]. | ||||||||||||
Name | SID 7969543 | ||||||||||||
CAS | 868224-64-0 | ||||||||||||
Formula | C24H24N2O7 | ||||||||||||
Molar Mass | 452.46 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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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. |