Art. -Nr.: HY-131364

Nur77 modulator 1

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Nur77 modulator 1 is a good Nur77 binder (K_D = 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.

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Reinheit: 98.16%
CAS. Nr.: 2469975-55-9
Formel: C₂₈H₂₅N₅O₂S
Molecular Weight:495.60

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Nur77 modulator 1 Chemical Structure

CAS. Nr.: 2469975-55-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Nur77/NR4A1

Alle Nuclear Hormone Receptor 4A/NR4A Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	0.6 μM Compound: 10g	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32717483]
L02	IC₅₀	>20 μM Compound: 10g	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32717483]
QGY-7703	IC₅₀	0.89 μM Compound: 10g	Antiproliferative activity against human QGY-7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human QGY-7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32717483]
SMMC-7721	IC₅₀	1.4 μM Compound: 10g	Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32717483]

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)^[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC₅₀ 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS. Nr. 2469975-55-9
Appearance Solid
Molecular Weight 495.60
Formel C₂₈H₂₅N₅O₂S
Color White to yellow
SMILES

CC1=NC2=C(OC)C=CC=C2C(NC3=CC4=C(NC(C(N/N=C/C5=CC=C(SC)C=C5)=O)=C4)C=C3)=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (252.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0178 mL

10.0888 mL

20.1776 mL

5 mM

0.4036 mL

2.0178 mL

4.0355 mL

10 mM

0.2018 mL

1.0089 mL

2.0178 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.20 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0178 mL	10.0888 mL	20.1776 mL	50.4439 mL
	5 mM	0.4036 mL	2.0178 mL	4.0355 mL	10.0888 mL
	10 mM	0.2018 mL	1.0089 mL	2.0178 mL	5.0444 mL
	15 mM	0.1345 mL	0.6726 mL	1.3452 mL	3.3629 mL
	20 mM	0.1009 mL	0.5044 mL	1.0089 mL	2.5222 mL
	25 mM	0.0807 mL	0.4036 mL	0.8071 mL	2.0178 mL
	30 mM	0.0673 mL	0.3363 mL	0.6726 mL	1.6815 mL
	40 mM	0.0504 mL	0.2522 mL	0.5044 mL	1.2611 mL
	50 mM	0.0404 mL	0.2018 mL	0.4036 mL	1.0089 mL
	60 mM	0.0336 mL	0.1681 mL	0.3363 mL	0.8407 mL
	80 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6305 mL
	100 mM	0.0202 mL	0.1009 mL	0.2018 mL	0.5044 mL

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Nur77 modulator 1

Apoptosis Compound Library

Anti-Cancer Compound Library

Endoplasmic Reticulum Stress Compound Library

Anti-Liver Cancer Compound Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alle Nuclear Hormone Receptor 4A/NR4A Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nur77 modulator 1

Apoptosis Compound Library

Anti-Cancer Compound Library

Endoplasmic Reticulum Stress Compound Library

Anti-Liver Cancer Compound Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alle Nuclear Hormone Receptor 4A/NR4A Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nur77 modulator 1 Related Classifications

HY-131364 Related Classifications