SID 7969543 - CAS 868224-64-0
Category: Inhibitor
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Molecular Formula:
C24H24N2O7
Molecular Weight:
452.46
COA:
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Targets:
Others
Description:
SID 7969543 is a selective steroidogenic factor-1 (SF-1, NR5A1) inhibitor (IC50 = 0.76, >33 and >33 μM at SF-1, RORα and VP16, respectively). It also inhibits SF-1-dependent luciferase expression in HEK 293T cells in vitro (IC50 = 30 nM).
Brife Description:
SF-1/NR5A1 inhibitor
Purity:
≥98% by HPLC
Synonyms:
SID 7969543; SID7969543; SID-7969543; Ethyl 2-[[2-[2-[(2,3-Dihydro-1,4-benzodioxin-6-yl)amino]-2-oxoethyl]-1,2-dihydro-1-oxo-5-isoquinolinyl]oxy]propanoate
MSDS:
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InChIKey:
KWMBIIQCLUIHDI-UHFFFAOYSA-N
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)
Canonical SMILES:
CCOC(=O)C(C)OC1=CC=CC2=C1C=CN(C2=O)CC(=O)NC3=CC4=C(C=C3)OCCO4
1.Potent, selective and cell penetrant inhibitors of SF-1 by functional ultra-high-throughput screening.
Madoux F;Li X;Chase P;Zastrow G;Cameron MD;Conkright JJ;Griffin PR;Thacher S;Hodder P Mol Pharmacol. 2008 Jun;73(6):1776-84. doi: 10.1124/mol.108.045963. Epub 2008 Mar 11.
The steroidogenic factor 1 (SF-1, also known as NR5A1) is a transcription factor belonging to the nuclear receptor superfamily. Whereas most of the members of this family have been extensively characterized, the therapeutic potential and pharmacology of SF-1 still remains elusive. Described here is the identification and characterization of selective inhibitory chemical probes of SF-1 by a rational ultra-high-throughput screening (uHTS) strategy. A set of 64,908 compounds from the National Institute of Health's Molecular Libraries Small Molecule Repository was screened in a transactivation cell-based assay employing a chimeric SF-1 construct. Two analogous isoquinolinones, ethyl 2-[2-[2-(2,3-dihydro-1,4-benzodioxin-7-ylamino)-2-oxoethyl]-1-oxoisoquinolin-5-yl]oxypropanoate (SID7969543) and ethyl 2-[2-[2-(1,3-benzodioxol-5-ylmethylamino)-2-oxoethyl]-1-oxoisoquinolin-5-yl]oxypropanoate and (SID7970631), were identified as potent submicromolar inhibitors, yielding IC(50) values of 760 and 260 nM. The compounds retained their potency in a more physiologic functional assay employing the full-length SF-1 protein and its native response element, yielding IC(50) values of 30 and 16 nM, respectively.
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CAS 868224-64-0 SID 7969543

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