Ferroptosis inducer-18
Ferroptosis inducer-18 is a ferroptosis inducer targeting NQO1. Ferroptosis inducer-18 acts as an NQO1 substrate, undergoes redox cycling, and produces partial cytotoxicity. Ferroptosis inducer-18 induces ROS generation, triggering lipid peroxidation and DNA damage. Ferroptosis inducer-18 exhibits selective cytotoxicity against prostate cancer cells, causing increased cytoplasmic volume, vacuolization, and loss of membrane integrity in prostate cancer cells. Ferroptosis inducer-18 can be used in prostate cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 2925251-41-6
- Formula: C34H26N4O6
- Molecular Weight:586.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
NQO1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | IC50 |
0.97 μM
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Cytotoxicity against human DU-145 prostate cancer cells assessed as viability reduction after 24 hrs by MTT assay.
Cytotoxicity against human DU-145 prostate cancer cells assessed as viability reduction after 24 hrs by MTT assay.
|
acsomega.5c11250 |
| DU-145 | IC50 |
1.04 μM
|
Cytotoxicity against human DU-145 prostate cancer cells assessed as viability reduction after 48 hrs by MTT assay.
Cytotoxicity against human DU-145 prostate cancer cells assessed as viability reduction after 48 hrs by MTT assay.
|
acsomega.5c11250 |
| DU-145 | IC50 |
0.96 μM
|
Cytotoxicity against human DU-145 prostate cancer cells assessed as viability reduction after 72 hrs by MTT assay.
Cytotoxicity against human DU-145 prostate cancer cells assessed as viability reduction after 72 hrs by MTT assay.
|
acsomega.5c11250 |
| MRC5 | IC50 |
3.90 μM
|
Cytotoxicity against human MRC-5 nontumor fibroblasts assessed as viability reduction after 24 hrs by MTT assay.
Cytotoxicity against human MRC-5 nontumor fibroblasts assessed as viability reduction after 24 hrs by MTT assay.
|
acsomega.5c11250 |
| MRC5 | IC50 |
3.79 μM
|
Cytotoxicity against human MRC-5 nontumor fibroblasts assessed as viability reduction after 48 hrs by MTT assay.
Cytotoxicity against human MRC-5 nontumor fibroblasts assessed as viability reduction after 48 hrs by MTT assay.
|
acsomega.5c11250 |
| MRC5 | IC50 |
3.60 μM
|
Cytotoxicity against human MRC-5 nontumor fibroblasts assessed as viability reduction after 72 hrs by MTT assay.
Cytotoxicity against human MRC-5 nontumor fibroblasts assessed as viability reduction after 72 hrs by MTT assay.
|
acsomega.5c11250 |
In Vitro
Ferroptosis inducer-18 (compound 4) acts as an NQO1 substrate with a relative enzymatic activity of 76.96% and forms an NQO1 complex with a melting temperature of 51.78 °C[1].
Ferroptosis inducer-18 (0.098-12.5 μM; 24-72 h) exhibits potent and time-independent cytotoxicity in DU-145 prostate cancer cells and is selective against MRC-5 fibroblasts[1].
Ferroptosis inducer-18 (0.5-1 μM; 24 h) reduced DU-145 cell density and membrane integrity in a concentration-dependent manner, with viability decreasing to 48.83% at 1 μM[1].
Ferroptosis inducer-18 exhibits low hemolytic activity in mouse erythrocytes, with EC50 > 200 μM and a hemolysis rate of 1.04%[1].
Ferroptosis inducer-18 (24 h) cytotoxicity in DU-145 cells can be reduced by pre-incubation with NAC (HY-B0215) (5 mM), increasing the IC50 from 0.97 μM to 3.28 μM[1].
Ferroptosis inducer-18 (1 μM; 6 h) induced lipid peroxidation in DU-145 cells with an oxidation rate of 1.51[1].
Ferroptosis inducer-18 (0.04-12.5 μM; 24 h) exhibits cytotoxicity in DU-145 cells that is partially dependent on NQO1, with the IC50 increasing from 0.97 μM to 2.02 μM in the presence of Dicoumarol (HY-N0645), while remaining potent in NQO1-low-expressing HL-60 cells[1].
Ferroptosis inducer-18 (0.97 μM; 24 h) combined with deferoxamine rescue increased DU-145 cell viability, indicating the presence of iron-dependent ferroptosis[1].
Ferroptosis inducer-18 (3-24 h) induces ROS in DU-145 cells[1].
Ferroptosis inducer-18 (0.5-1 μM; 24 h) induces oxidative DNA damage in DU-145 cells, which is reduced by NAC and enhanced by hOGG1[1].
Ferroptosis inducer-18 (0.5-1 μM; 6-24 h) induces mitochondrial depolarization in DU-145 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:DU-145 prostate cancer cells
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Concentration:0.5, 1 μM
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Incubation Time:24 h
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Result:Caused increased cytoplasmic size.
Flow cytometry showed cellular densities of 13.71 × 10^4 cells/mL at 0.5 μM and 8.23 × 10^4 cells/mL at 1 μM.
Membrane integrity/viability was 83.37% at 0.5 μM and 48.83% at 1 μM.
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Cell Line:DU-145 prostate cancer cells
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Concentration:0.97 μM
50, 100 μM (DFO (HY-D0903)) -
Incubation Time:24 h
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Result:Gave 14.18% cell viability alone.
With DFO 50 μM, viability increased to 48.73%; with DFO 100 μM, viability increased to 62.54%.
DFO increased viability more than 3-fold compared with compound 4 alone.
Chemical Information
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CAS No. 2925251-41-6
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Molecular Weight 586.59
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Formula C34H26N4O6
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SMILES
CC1(OC2=C(C1N3C=C(N=N3)CNC4=CC(C5=C(C(OCC6=CC=CC=C6)=CC=C5)C4=O)=O)C(C(C7=CC=CC=C72)=O)=O)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Ferroptosis inducer-18
- 2925251-41-6
- Ferroptosis inducer18
- Ferroptosis inducer 18
- Reactive Oxygen Species (ROS)
- Quinone Reductase
- Ferroptosis
- DNA damage
- DU-145
- NQO1
- ferroptosis
- fibroblasts
- lipid peroxidation
- mitochondrial membrane depolarization
- oxidative stress
- prostate cancer
- reactive oxygen species
- Inhibitor
- inhibitor
- inhibit