Ferroptosis-IN-22
Based on 1 Customer Validation
Ferroptosis-IN-22 is a selective ferroptosis inhibitor by targeting NCOA4 and disrupting its interaction with ferritin with an EC50 of 520 nM and a Kd of 0.78 μM. Ferroptosis-IN-22 has a strong inhibitory activity against ferroptosis induced by multiple ferroptosis inducers (RSL3 (HY-100218A), Erastin (HY-15763), ML210 (HY-100003), FIN56 (HY-103087)), but does not inhibit necrosis induced by H2O2 or apoptosis induced by STS (HY-15141). Ferroptosis-IN-22 effectively ameliorates Concanavalin A (HY-P2149)-induced acute liver injury. Ferroptosis-IN-22 can be used for the study of ferroptosis-related diseases.
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- Purity : 99.95%
- CAS No.: 3096878-87-1
- 화학식: C27H23NO2
- 분자량:393.48
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보관:
Store at room temperature, keep dry and cool.
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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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
Ferroptosis-IN-22 (Compound 4k) exhibits anti-ferroptotic activity with EC50 values were 0.515 μM (RSL3) and 2.776 μM (Erastin) in HT-1080 cells, 0.4061 μM (RSL3) and 1.308 μM (Erastin) in 786-O cells, and 0.093 μM (RSL3) and 1.013 μM (Erastin) in MDA-MB-231 cells, and also suppresses ferroptosis induced by ML210 and FIN56[1].
Ferroptosis-IN-22 (4-8 μM) significantly reduced RSL3 or Erastin induced lipid peroxidation in both HT-1080 and 786-O cells and does not have direct antioxidative activity[1].
Ferroptosis-IN-22 (4 μM, 6 h) directly binds to NCOA4, a key receptor protein in ferritin autophagy, disrupting the interaction between NCOA4 and ferritin (FTH1), thereby inhibiting the ferritin autophagy process rather than relying on direct iron chelation in HT-1080 cells[1].
Ferroptosis-IN-22 demonstrates low cardiotoxicity and minimal risk of CYP-mediated drug-drug interactions (DDIs)[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 cells
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Concentration:4 μM
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Incubation Time:6 h
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Result:Significantly reduced the amount of FTH1/FTL co-precipitated with NCOA4.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | F | Vss | Vd | CL |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | p.o. | 3.751 h | 2.000 h | 557.082 ng/mL | 1474.816 ng·h/mL | 1498.461 ng·h/mL | 2.961 h | 3.263 h | 2.421 % | / | / | / |
| Rat[1] | 5 mg/kg | i.v. | 4.009 h | 0.083 h | 61139.150 ng/mL | 30464.355 ng·h/mL | 30509.903 ng·h/mL | 0.645 h | 0.689 h | / | 113.508 mL/kg | 941.525 mL/kg | 164.535 mL/h/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ConA induced acute liver injury model established in C57BL/6J mice[1]
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Dosage:5 and 15 mg/kg
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Administration:Intraperitoneal injection (i.p.), 24 hours and 0.5 hours before ConA injection
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Result:Decreased serum ALT and AST levels and improved liver tissue injury.
Significantly reduced the mRNA levels of TNF-α and IL-6, two major inflammatory cytokines in the liver.
Effectively reduced the levels of4-HNE and MDA, two lipid peroxidation products, in liver tissues.
Showed no effect on the morphology and the 4-HNE level of other vital organs including kidney, spleen, heart and lung.
Reduced the mRNA expression of ferroptosis marker Ptgs2.
Chemical Information
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CAS No. 3096878-87-1
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Appearance Solid
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분자량 393.48
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화학식 C27H23NO2
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Color White to off-white
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SMILES
CC(C)(C1=C(O)C=C2C(C(C(C3=CC=CC=C3)=C4)=C(O2)N=C4C5=CC=CC=C5)=C1)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Store at room temperature, keep dry and cool
In solvent -80°C 1 year -20°C 6 months
용액&용해도
In Vitro:
DMSO : 100 mg/mL (254.14 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 2.5 mg/mL (6.35 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.
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: ≥ 2.5 mg/mL (6.35 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 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.
Protocol
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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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
순도&문서
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.5414 mL | 12.7071 mL | 25.4143 mL | 63.5356 mL |
| 5 mM | 0.5083 mL | 2.5414 mL | 5.0829 mL | 12.7071 mL | |
| 10 mM | 0.2541 mL | 1.2707 mL | 2.5414 mL | 6.3536 mL | |
| 15 mM | 0.1694 mL | 0.8471 mL | 1.6943 mL | 4.2357 mL | |
| 20 mM | 0.1271 mL | 0.6354 mL | 1.2707 mL | 3.1768 mL | |
| 25 mM | 0.1017 mL | 0.5083 mL | 1.0166 mL | 2.5414 mL | |
| 30 mM | 0.0847 mL | 0.4236 mL | 0.8471 mL | 2.1179 mL | |
| 40 mM | 0.0635 mL | 0.3177 mL | 0.6354 mL | 1.5884 mL | |
| 50 mM | 0.0508 mL | 0.2541 mL | 0.5083 mL | 1.2707 mL | |
| 60 mM | 0.0424 mL | 0.2118 mL | 0.4236 mL | 1.0589 mL | |
| 80 mM | 0.0318 mL | 0.1588 mL | 0.3177 mL | 0.7942 mL | |
| 100 mM | 0.0254 mL | 0.1271 mL | 0.2541 mL | 0.6354 mL |
Ferroptosis-IN-22 Related Classifications
HY-175869 Related Classifications
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