868224-64-0

868224-64-0 structure

Name: SID 7969543
Chemical Name: ethyl 2-[2-[2-(2,3-dihydro-1,4-benzodioxin-6-ylamino)-2-oxoethyl]-1-oxoisoquinolin-5-yl]oxypropanoate
CAS Number: 868224-64-0
Molecular Formula: C₂₄H₂₄N₂O₇
Molecular Weight: 452.45700
Catalog: Research Areas Endocrinology
Create Date: 2017-07-03 05:29:49
Modify Date: 2024-01-12 13:45:42
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].

Name	ethyl 2-[2-[2-(2,3-dihydro-1,4-benzodioxin-6-ylamino)-2-oxoethyl]-1-oxoisoquinolin-5-yl]oxypropanoate
Synonyms	F1808-0160 isoquinolinone scaffold,2

Description	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].
Related Catalog	Research Areas >> Endocrinology Signaling Pathways >> Others >> Others
In Vitro	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].
References	[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.

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes	Xi
RIDADR	NONH for all modes of transport

1030880-15-9

22013-33-8

868224-64-0

Precursor 1
22013-33-8
DownStream 0