Chemical Structure : Nur77 antagonist ja
CAS No.:
2378780-25-5
Nur77 antagonist ja
Catalog No.: PC-21509Not For Human Use, Lab Use Only.
Nur77 antagonist ja is a potent, selective antagonist of the orphan nuclear receptor Nur77 (NGFIB, TR3, SPR Kd=91 nM), exhibits antiproliferative activity against MDA-MB-231 cells with IC50 of 0.4 uM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Nur77 antagonist ja is a potent, selective antagonist of the orphan nuclear receptor Nur77 (NGFIB, TR3, SPR Kd=91 nM), exhibits antiproliferative activity against MDA-MB-231 cells with IC50 of 0.4 uM.
Nur77 antagonist ja exhibits excellent antiproliferative activity against breast cancer cell lines (MDA-MB-231 and T47D, IC50 < 1.2 μM), and the human cervical cancer cell line (HeLa, IC50=1.99 uM).
Nur77 antagonist ja binds to Nur77-LBD directly and effectively with Kd of 154 nM in fuorescence titration analysis, inhibits its transcriptional activity.
Nur77 antagonist ja (2 uM) significantly induces Nur77-dependent apoptosis in MDA-MB-231 cell via a caspase-dependent pathway by mediating the TP53 phosphorylation pathway.
Nur77 antagonist ja significantly suppressed MDA-MB-231 xenograft tumor growth but had no apparent side effects in mice and zebrafish.
Physicochemical Properties
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M.Wt
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492.65
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Formula
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C25H32N8OS
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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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N-(3-(Diethylamino)propyl)-5-((4-(4-methyl-2-(methylamino)thiazol-5-yl) Pyrimidin-2-yl)amino)-1H-indole-2-carboxamide
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References
1. Jingbo Qin, et al. Journal of Medicinal Chemistry, 2023
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