NR5A2 inhibitor Cmp3

Chemical Structure : NR5A2 inhibitor Cmp3

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货号: PC-21458Not For Human Use, Lab Use Only.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
200 mg		Get quote
1 g		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	375.47
分子式	C23H25N3O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(3'-{1-[2-(4-morpholinyl)ethyl]-1H-pyrazol-3-yl}-3-biphenylyl)ethanone

参考文献

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.