Art. -Nr.: HY-113848

AEM1

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AEM1 is an Nrf2 inhibitor with anti-tumor and oral activity. AEM1 promotes the differentiation of HepaRG cells towards mature liver cells, aiding in the recovery of damaged liver.

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Reinheit: 99.83%
CAS. Nr.: 1030123-90-0
Formel: C₂₀H₁₄FN₃O₂S
Molecular Weight:379.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AEM1 Chemical Structure

CAS. Nr.: 1030123-90-0

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

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

Biologische Aktivität

Beschreibung

AEM1 is an Nrf2 inhibitor with anti-tumor and oral activity. AEM1 promotes the differentiation of HepaRG cells towards mature liver cells, aiding in the recovery of damaged liver^[1]^[2].

In Vitro

AEM1 (0.625-10 μM, 24 h) inhibits ARE-LUC signaling and HMOX1 in A549 cells^[1].
AEM1 (5 μM, 72 h) suppresses NRF2 activity in A549 cells^[1].
AEM1 (0-5 μM, 24 h) causes a dose-dependent decrease in the levels of reduced glutathione (GSH) in A549 cells^[1].
AEM1 (0-10 μM, 48-72 h) reduces the growth capability of A549 cells under anchorage-independent conditions, and when combined with etoposide and 5-fluorouracil, it enhances the toxicity of these two chemotherapeutic drugs on A549 cells, making them more sensitive to hydrogen peroxide-induced cell death^[1].
AEM1 (1-10 μM, 24 h) inhibition of NRF2 activity is limited to cell lines where the NRF2 transcriptional program is constitutively activated due to mutations^[1].
AEM1 (used at 1 μM dissolved in culture medium) inhibits NRF2 and promotes the differentiation of HepaRG cells towards mature hepatocytes^[2].

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

Real Time qPCR^[1]

Cell Line:

A549
Concentration:

0.625, 2.5, 5, 10 μM; 5 μM
Incubation Time:

24 h; 72 h
Result:

Inhibited ARE-LUC signaling and HMOX1.
Reduced the expression of GCLM, SOD1, TXN, HMDX1, and GPX2.

Cell Viability Assay^[1]

Cell Line:

A549
Concentration:

0, 1, 5, 10 μM
Incubation Time:

24, 72 h
Result:

Reduced proliferation capacity.

Real Time qPCR^[1]

Cell Line:

H838, H460, HEK293T, HeLa, SH-SY5Y, HLF
Concentration:

1, 10 μM
Incubation Time:

24 h
Result:

Showed that some cell types (such as HeLa and HEK293T cell lines) showed a slight repression of HMOX1 transcription levels, while other cell types (such as SH-SY5Y and human primary lung fibroblasts) showed a slight but reproducible upregulation trend of HMOX1 transcription levels.

Real Time qPCR^[2]

Cell Line:

HepaRG2
Concentration:

1 μM
Incubation Time:

1 μM dissolved in culture medium for use
Result:

Increased expression of albumin, CYP3A4, and GGT1 genes, and increased expression of CD49a and cd49f.

In Vivo

AEM1 (50 mg/kg, oral, twice daily, 20 days) inhibits tumor proliferation in the subcutaneous A549 mouse model^[1].
Pharmacokinetic Analysis in Mice^[1]

Route	Dose (mg/kg)	AUC_0-24 (ng•h/mL)	t_1/2 (h)	C_max (ng/mL)
Oral	20	453	2	176

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

Animal Model:

Mouse model of subcutaneous transplantation of A549^[1]
Dosage:

50 mg/kg; twice a day; 20 days
Administration:

Oral
Result:

Inhibited tumor proliferation.

Chemical Information

CAS. Nr. 1030123-90-0
Appearance Solid
Molecular Weight 379.41
Formel C₂₀H₁₄FN₃O₂S
Color White to off-white
SMILES

FC1=CC=C(C2=CSC3=NC=NC(NCC4=CC=C(OCO5)C5=C4)=C32)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (263.57 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

2.6357 mL

13.1784 mL

26.3567 mL

5 mM

0.5271 mL

2.6357 mL

5.2713 mL

10 mM

0.2636 mL

1.3178 mL

2.6357 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. 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: 2.5 mg/mL (6.59 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 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 (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. DeNicola GM, et al. Oncogene-induced Nrf2 transcription promotes ROS detoxification and tumorigenesis. Nature. 2011 Jul 6;475(7354):106-9. [Content Brief]

[2]. Bollong MJ, Yun H, Sherwood L, Woods AK, Lairson LL, Schultz PG. A Small Molecule Inhibits Deregulated NRF2 Transcriptional Activity in Cancer. ACS Chem Biol. 2015 Oct 16;10(10):2193-8. [Content Brief]

[3]. Francesco Bellanti, et al. Inhibition of nuclear factor (erythroid-derived 2)-like 2 promotes hepatic progenitor cell activation and differentiation [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

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6357 mL	13.1784 mL	26.3567 mL	65.8918 mL
	5 mM	0.5271 mL	2.6357 mL	5.2713 mL	13.1784 mL
	10 mM	0.2636 mL	1.3178 mL	2.6357 mL	6.5892 mL
	15 mM	0.1757 mL	0.8786 mL	1.7571 mL	4.3928 mL
	20 mM	0.1318 mL	0.6589 mL	1.3178 mL	3.2946 mL
	25 mM	0.1054 mL	0.5271 mL	1.0543 mL	2.6357 mL
	30 mM	0.0879 mL	0.4393 mL	0.8786 mL	2.1964 mL
	40 mM	0.0659 mL	0.3295 mL	0.6589 mL	1.6473 mL
	50 mM	0.0527 mL	0.2636 mL	0.5271 mL	1.3178 mL
	60 mM	0.0439 mL	0.2196 mL	0.4393 mL	1.0982 mL
	80 mM	0.0329 mL	0.1647 mL	0.3295 mL	0.8236 mL
	100 mM	0.0264 mL	0.1318 mL	0.2636 mL	0.6589 mL

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AEM1

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Orally Active Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Anti-Ovarian Cancer Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AEM1

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Orally Active Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Anti-Ovarian Cancer Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AEM1 Related Classifications

HY-113848 Related Classifications