1. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Ferroptosis Reactive Oxygen Species (ROS)
  3. Ferroptosis-IN-21

Ferroptosis-IN-21  (Synonyms: 1,2,3,4-Tetrahydroquinolin-8-ol; 8-hydroxy-1,2,3,4-tetrahydroquinoline)

Cat. No.: HY-W002942
Handling Instructions Technical Support

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.

Ferroptosis-IN-21

Ferroptosis-IN-21 Chemical Structure

CAS No. : 6640-50-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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[1].

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.

Cell Viability Assay[1]

Cell Line: HT-1080, HKC and HK-2 cells
Concentration: 0.01-10 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: HKC cells
Concentration: 500 nM
Incubation Time: 24 h
Result: Did not significantly alter GPX4 protein expression in either untreated or RSL3- stimulated cells.
In Vivo

Ferroptosis-IN-21 (5 and 10 mg/kg, i.p., 24 hours and 1 hour pre-treatment) shows potent renoprotective effects against ischemic acute kidney injury (AKI) in a renal ischemia-reperfusion mice model[1].

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

Animal Model: Male C57BL/6 mice (8-12 weeks old) subjected to bilateral renal ischemia (40 min) and reperfusion (24 h) [1]
Dosage: 5 and 10 mg/kg
Administration: i.p., 24 hours and 1 hour pre-treatment
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.
Molecular Weight

149.19

Formula

C9H11NO

CAS No.
Appearance

Solid

SMILES

OC1=CC=CC2=C1NCCC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

RT, protect from light

In solvent -80°C 2 years
-20°C 1 year
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.7029 mL 33.5143 mL 67.0286 mL
5 mM 1.3406 mL 6.7029 mL 13.4057 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    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.
  • Protocol 2

    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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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
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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.

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