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Nur77 modulator 1

Catalog No. T40130   CAS 2469975-55-9
Synonyms: Nur77 modulator 1

Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Nur77 modulator 1 shows anti-hepatoma activity.

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Nur77 modulator 1 Chemical Structure
Nur77 modulator 1, CAS 2469975-55-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 116.00
5 mg In stock $ 288.00
10 mg In stock $ 478.00
25 mg In stock $ 789.00
50 mg In stock $ 1,080.00
100 mg In stock $ 1,480.00
500 mg In stock $ 2,970.00
1 mL * 10 mM (in DMSO) In stock $ 315.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Nur77 modulator 1 shows anti-hepatoma activity.
Targets&IC50 Nur77:3.58 μM (KD)
In vitro Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines which are HepG2, QGY-7703, and SMMC-7721 respectively, and less cytotoxicity against LO2 cells (human normal liver cell line) [1]. Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner [1]. Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis [1] . Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete) [1] . Cell Viability Assay [1] . Cell Line: Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721). Concentration: 0-20 μM. Incubation Time: 12-24 hours. Result: Exhibited IC 50 values of 0.6 μM, 0.89 μM, 1.40 μM and >20 μM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively. Reduced the viability in a time-dependent manner. Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.
In vivo Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability [1]. Animal Model: Nude mouse hepatoma HepG2 xenograft [1]. Dosage: 10 and 20 mg/kg/day. Administration: IP, once every day for 15 days. Result: Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice. These results indicate that Nur77 modulator 1 has the potential to be developed as a novel Nur77-targeting anti-hepatoma drug.
Synonyms Nur77 modulator 1
Molecular Weight 495.6
Formula C28H25N5O2S
CAS No. 2469975-55-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (252.22 mM), sonification is recommended.

TargetMolReferences and Literature

1. Baicun Li, et al. Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators. Eur J Med Chem. 2020 Oct 15;204:112608.

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Keywords

Nur77 modulator 1 2469975-55-9 Others apoptosis inhibit Inhibitor antitumor Nur-77 modulator 1 tolerability autophagy stress mitochondria good inhibitor

 

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