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Chemical Structure : 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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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.
| M.Wt | 375.47 | |
| Formula | C23H25N3O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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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