Ferroptosis-IN-21
Based on 1 Customer Validation
Ferroptosis-IN-21 is a ferroptosis inhibitor that protects against renal I/R injury by suppressing ferroptosis and directly scavenging peroxyl radicals. Ferroptosis-IN-21 displays broad-spectrum anti-ferroptotic efficacy across multiple inducers in renal tubular epithelial cells, with nanomolar potency and robust suppression of lipid Reactive Oxygen Species (ROS). Ferroptosis-IN-21 significantly ameliorates renal I/R injury in mice, reducing histological damage, functional impairment, and inflammatory cytokine expression, while decreasing lipid peroxidation biomarkers such as 4-hydroxynonenal. Ferroptosis-IN-12 can be used for research in the field of ferroptosis-targeted drug development.
For research use only. We do not sell to patients.
- Purity : 99.88%
- CAS No.: 6640-50-2
- Formula: C9H11NO
- Molecular Weight:149.19
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Storage:
RT, protect from light.
In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-W000806
ThallineTetrahydroquinoline Derivative -
HY-107870
1,2,4-Triazole-3-carboxylic acid, 97%Biochemical Assay Reagent -
HY-W250457
Ondansetron impurity 6Drug Impurity -
HY-W338780
Cyclohexane-1,2,3,4,5,6-hexacarboxylic acidMetal-organic Framework -
HY-W250457R
9-Methyl-3-methylene-2,3-dihydro-1H-carbazol-4(9H)-one (Standard) -
HY-W040960R
H-1,2,4-Triazole-3-carboxamide (Standard)
Biological Activity
Description
In Vitro
Ferroptosis-IN-21 (compound 6) (0.01-10 μM, 24 h) exhibits nanomolar cytoprotective activity (EC50 = 61.7 nM) and completely reverses cell death at 200 nM in HT-1080 cells, and dose-dependently protects Human Kidney Cortex epithelial cells (HKC) and Human Kidney 2 (HK-2) cells from ferroptosis induced by RSL-3 (HY-100218A) and FIN-56, confirming its broad-spectrum efficacy[1].
Ferroptosis-IN-21 (50-500 nM, 24 h) significantly suppresses RSL-3-induced lipid ROS accumulation and MDA elevation, and has no effect on GPX4 protein levels[1].
Ferroptosis-IN-21 (10 µM) does not chelate iron ions, ruling out an iron-chelating mechanism[1].
Ferroptosis-IN-21 (1-80 µM, 30 min) exhibits potent direct radical scavenging activity in Cell-free DPPH assay[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:HT-1080, HKC and HK-2 cells
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Concentration:0.01-10 μM
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Incubation Time:24 h
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Result:Exhibited nanomolar cytoprotective activity with an EC50 of 61.7 nM in HT-1080 cells.
Completely reversed RSL3-induced cell death in HT-1080 cells at the dose of 200 nM.
Exhibited significant cytoprotective effects on both HKC and HK-2 cells under RSL3-induced ferroptosis, displaying a concentration-dependent relationship, with the EC50 values of 361 and 258 nM, respectively.
Effectively inhibited FIN56-induced cell death in both HKC and HK-2 cells.
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Cell Line:HKC cells
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Concentration:500 nM
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Incubation Time:24 h
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Result:Did not significantly alter GPX4 protein expression in either untreated or RSL3- stimulated cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (8-12 weeks old) subjected to bilateral renal ischemia (40 min) and reperfusion (24 h) [1]
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Dosage:5 and 10 mg/kg
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Administration:i.p., 24 hours and 1 hour pre-treatment
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Result:Reduced the serum creatinine, blood urea nitrogen (BUN), and kidney coefficient relative to the I/R group.
Conferred substantial structural protection, with the 10 mg/kg dose yielding the most notable histological preservation.
Markedly suppressed mRNA expression levels of KIM-1 and NGAL in a dose-dependent manner.
Significantly reduced the expression of TNF-α, IL1-β, IL-6, and MCP-1 upregulated by I/R insult in a dose-dependent manner, indicating an anti-inflammatory effect.
Markedly reduced I/R-induced 4-HNE accumulation.
Chemical Information
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CAS No. 6640-50-2
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Appearance Solid
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Molecular Weight 149.19
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Formula C9H11NO
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Color Off-white to yellow
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SMILES
OC1=CC=CC2=C1NCCC2
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Synonyms
1,2,3,4-Tetrahydroquinolin-8-ol; 8-hydroxy-1,2,3,4-tetrahydroquinoline
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
RT, protect from light
In solvent -80°C 1 year -20°C 6 months
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (670.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (33.51 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (33.51 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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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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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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Data Sheet (283 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 6.7029 mL | 33.5143 mL | 67.0286 mL | 167.5716 mL |
| 5 mM | 1.3406 mL | 6.7029 mL | 13.4057 mL | 33.5143 mL | |
| 10 mM | 0.6703 mL | 3.3514 mL | 6.7029 mL | 16.7572 mL | |
| 15 mM | 0.4469 mL | 2.2343 mL | 4.4686 mL | 11.1714 mL | |
| 20 mM | 0.3351 mL | 1.6757 mL | 3.3514 mL | 8.3786 mL | |
| 25 mM | 0.2681 mL | 1.3406 mL | 2.6811 mL | 6.7029 mL | |
| 30 mM | 0.2234 mL | 1.1171 mL | 2.2343 mL | 5.5857 mL | |
| 40 mM | 0.1676 mL | 0.8379 mL | 1.6757 mL | 4.1893 mL | |
| 50 mM | 0.1341 mL | 0.6703 mL | 1.3406 mL | 3.3514 mL | |
| 60 mM | 0.1117 mL | 0.5586 mL | 1.1171 mL | 2.7929 mL | |
| 80 mM | 0.0838 mL | 0.4189 mL | 0.8379 mL | 2.0946 mL | |
| 100 mM | 0.0670 mL | 0.3351 mL | 0.6703 mL | 1.6757 mL |
Ferroptosis-IN-21 Related Classifications
HY-W002942 Related Classifications
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Keywords
- Ferroptosis-IN-21
- 6640-50-2
- 1,2,3,4-Tetrahydroquinolin-8-ol
- 8-hydroxy-1,2,3,4-tetrahydroquinoline
- Free Radical Scavengers
- Ferroptosis
- Reactive Oxygen Species (ROS)
- ferroptosis
- AKT
- renal I/R injury
- peroxyl radicals
- anti-ferroptotic
- renal tubular epithelial cells
- ROS
- histological damage
- inflammatory cytokine expression
- lipid peroxidation biomarkers
- renal ischemia-reperfusion mice model
- HT-1080
- HKC
- HK-2
- Inhibitor
- inhibitor
- inhibit