2. NF-κB Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation Autophagy
  3. Keap1-Nrf2 Ferroptosis Reactive Oxygen Species (ROS) Atg8/LC3
  4. Nrf2-IN-4

Nrf2-IN-4 is a Nrf2 inhibitor. Nrf2-IN-4 induces ferroptosis via NRF2 inhibition. Nrf2-IN-4 disrupts cellular iron homeostasis, facilitates ferritin degradation, and ultimately triggers ferroptosis. Nrf2-IN-4 induces lysosome activation by promoting iron-dependent ROS production and lysosomal acidification. Nrf2-IN-4 demonstrates significant antitumor efficacy. Nrf2-IN-4 can be used for the study of breast cancer.

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Nrf2-IN-4 Chemical Structure

Nrf2-IN-4 Chemical Structure

CAS No. : 2417486-06-5

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Nrf2-IN-4 Related Antibodies

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Description

Nrf2-IN-4 is a Nrf2 inhibitor. Nrf2-IN-4 induces ferroptosis via NRF2 inhibition. Nrf2-IN-4 disrupts cellular iron homeostasis, facilitates ferritin degradation, and ultimately triggers ferroptosis. Nrf2-IN-4 induces lysosome activation by promoting iron-dependent ROS production and lysosomal acidification. Nrf2-IN-4 demonstrates significant antitumor efficacy. Nrf2-IN-4 can be used for the study of breast cancer[1].

In Vitro

Nrf2-IN-4 (Compound PhcY) (0.01-10 μM, 72 h) exhibits inhibitory effect on the cancer cell lines, with IC50s of 80 nM (MCF-7 cells), 3.26 μM (HepG2 cells), 0.90 μM (T24 cells), 2.89 μM (HCT116 cells), 3.27 μM (L929 fibroblasts) and 5.36 μM (HEK293 human embryonic kidney cells)[1].
Nrf2-IN-4 (40-160 nM) causes MCF-7 cells to exhibit ‘ballooning’ and rounded cell morphology with vacuolated cytosol[1].
Nrf2-IN-4 (40-80 nM, 14 days) inhibits colony formation of MCF-7 cells in a dose-dependent manner[1].
Nrf2-IN-4 (80-160 nM, 24-48 h) increases labile iron pool (LIP) and ferroptosis via inhibition of Nrf2 in MCF-7 cells[1].
Nrf2-IN-4 (80-320 nM, 24 h) induces lysosome activation by promoting iron-dependent ROS production and lysosomal acidification in MCF-7 cells[1].
Nrf2-IN-4 (40-320 nM, 0-12 h) induces ferritin degradation via ferritinophagy in MCF-7 cells[1].
Nrf2-IN-4 (80-320 nM) induces oxidative stress, resulting in a significant decrease in mitochondrial membrane potential, an effect that can be reduced by the Acetylcysteine (N-acetylcysteine) (NAC) (HY-B0215) in MCF-7 cells[1].
Nrf2-IN-4 (0.1-0.2 μM) demonstrates a potent inhibitory effect on organoid growth, surpassing the efficacy of ML385(HY-100523)[1].

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

Nrf2-IN-4 Related Antibodies

Immunofluorescence[1]

Cell Line: MCF-7 cells
Concentration: 80 nM
Incubation Time: 24 h
Result: Increased LIP and reversed the effect and the the effect was reversed by Nrf2knockdown.

Cell Viability Assay[1]

Cell Line: MCF-7 cells
Concentration: 80, 160 nM
Incubation Time: 48 h
Result: Increased cytotoxicity upon Nrf2 overexpression.
Induced dose-dependent cytotoxicity, which was inhibited by both 1,8-Diazafluoren-9-one (DFO) (HY-D0903) and Ferrostatin-1 (Fer-1) (HY-100579).

Immunofluorescence[1]

Cell Line: MCF-7 cells
Concentration: 80, 160, 320 nM
Incubation Time: 24 h
Result: Increased cathepsin B activity in a dose-dependent manner, which was inhibited by Chloroquine (CQ)(HY-17589A) or DFO.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0, 3, 6, 9, 12 h
Incubation Time: 24 h
Result: Showed a dose-dependent increase in Beclin-1, LC3-II, and ATG5 protein levels.
Reduced intracellular FTH and FTL levels, and this reduction was reversed by autophagy inhibitors(Bafilomycin A1(HY-100558) ,CQ) and the iron chelator DFO.
In Vivo

Nrf2-IN-4 (Compound PhcY) (10 mg/kg, i.p., daily for 21 days) demonstrates significant antitumor efficacy in MCF-7 xenograft mice[1].

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

Animal Model: MCF-7 cells (5 × 106) were injected subcutaneously into each female adult athymic nude mouse [1]
Dosage: 10 mg/kg
Administration: i.p. daily for 21 days
Result: Led to the degradation of FTH and FTL, as well as the upregulation of P53 and LC3-II.
Did not cause notable body weight loss or other observable adverse effects in mice.
Molecular Weight

426.32

Formula

C20H13Cl2N5S
CAS No.
SMILES

ClC1=C(Cl)C=C(C2=CSC(N/N=C(C3=CC=CC=N3)/C4=NC=CC=C4)=N2)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Nrf2-IN-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nrf2-IN-42417486-06-5Keap1-Nrf2FerroptosisReactive Oxygen Species (ROS)Atg8/LC3Autophagy-related 8| ferroptosisbreast cancerROSMCF-7 cellsInhibitorinhibitorinhibit

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