Nur77 antagonist ja

Chemical Structure : Nur77 antagonist ja

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货号: PC-21509Not 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

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.

物理化学性质&存储条件

分子量	492.65
分子式	C25H32N8OS
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	N-(3-(Diethylamino)propyl)-5-((4-(4-methyl-2-(methylamino)thiazol-5-yl) Pyrimidin-2-yl)amino)-1H-indole-2-carboxamide

参考文献

1. Jingbo Qin, et al. Journal of Medicinal Chemistry, 2023