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Chemical Structure : 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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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.
| M.Wt | 492.65 | |
| Formula | C25H32N8OS | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jingbo Qin, et al. Journal of Medicinal Chemistry, 2023
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