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. Anti-hepatoma activity.
Product information
CAS Number: 2469975-55-9
Molecular Weight: 495.60
Formula: C28H25N5O2S
Chemical Name: 5-[(8-methoxy-2-methylquinolin-4-yl)amino]-N'-[(1E)-[4-(methylsulfanyl)phenyl]methylidene]-1H-indole-2-carbohydrazide
Smiles: CC1C=C(NC2=CC3C=C(NC=3C=C2)C(=O)N/N=C/C2C=CC(=CC=2)SC)C2=CC=CC(OC)=C2N=1
InChiKey: ZDSQJUKYFCIYLG-MUFRIFMGSA-N
InChi: InChI=1S/C28H25N5O2S/c1-17-13-24(22-5-4-6-26(35-2)27(22)30-17)31-20-9-12-23-19(14-20)15-25(32-23)28(34)33-29-16-18-7-10-21(36-3)11-8-18/h4-16,32H,1-3H3,(H,30,31)(H,33,34)/b29-16+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (252.22 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line). Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner. Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis. 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).
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.
Products are for research use only. Not for human use.
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