Chemical Structure : NR5A2 inhibitor Cmp3
CAS No.:
1185410-60-9
NR5A2 inhibitor Cmp3
Catalog No.: PC-21458Not For Human Use, Lab Use Only.
NR5A2 inhibitor Cpd3 is a specific small molecule inhibitor of NR5A2 (liver receptor homolog-1, LRH-1) with Kd of 1.5 uM in Biacore-based assays, inhibits the transcriptional activity of hLRH-1 with IC50 of 5 uM (G0S2 mRNA level).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
NR5A2 inhibitor Cpd3 is a specific small molecule inhibitor of NR5A2 (liver receptor homolog-1, LRH-1) with Kd of 1.5 uM in Biacore-based assays, inhibits the transcriptional activity of hLRH-1 with IC50 of 5 uM (G0S2 mRNA level).
NR5A2 inhibitor Cpd3 directly binds to LRH-1 LBD, diminishes the receptor's interactions with co-regulator DAX1–3 peptide in a dose-dependent manner.
NR5A2 inhibitor Cpd3 inhibits cancer cell proliferation in LRH-1-positive colon and breast cancer cells, inhibits transcription of LRH-1 target genes NR0B2 and CCNE1 (encoding SHP and cyclin E1).
NR5A2 inhibitor Cpd3 sensitizes a significant fraction of PDAC models derived from 18 patients to standard chemotherapy.
Physicochemical Properties
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M.Wt
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375.47
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Formula
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C23H25N3O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(3'-{1-[2-(4-morpholinyl)ethyl]-1H-pyrazol-3-yl}-3-biphenylyl)ethanone
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References
1. Cindy Benod, et al. J Biol Chem. 2013 Jul 5;288(27):19830-44.
2. Quan Zheng, et al. J Exp Clin Cancer Res. 2023 Nov 28;42(1):323.
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