1. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Ferroptosis Reactive Oxygen Species (ROS)
  3. Ferroptosis-IN-26

Ferroptosis-IN-26 is a CEPT1-targeting ferroptosis inhibitor. Ferroptosis-IN-26 enhances CEPT1-dependent phosphatidylcholine remodeling to enrich cellular membranes with monounsaturated fatty acid-containing phosphatidylcholine (PC-MUFA). Ferroptosis-IN-26 suppresses lipid peroxidation. Ferroptosis-IN-26 can be used for the research of acute liver injury.

For research use only. We do not sell to patients.

Ferroptosis-IN-26

Ferroptosis-IN-26 Chemical Structure

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Description

Ferroptosis-IN-26 is a CEPT1-targeting ferroptosis inhibitor. Ferroptosis-IN-26 enhances CEPT1-dependent phosphatidylcholine remodeling to enrich cellular membranes with monounsaturated fatty acid-containing phosphatidylcholine (PC-MUFA). Ferroptosis-IN-26 suppresses lipid peroxidation. Ferroptosis-IN-26 can be used for the research of acute liver injury[1].

In Vitro

Ferroptosis-IN-26 (Compound 4g) potently inhibits RSL3 (HY-100218A)-induced ferroptosis in 786-O cells with an EC50 of 0.16 μM[1].
Ferroptosis-IN-26 potently inhibits RSL3-induced ferroptosis in HT-1080 cells with an EC50 of 0.15 μM[1].
Ferroptosis-IN-26 potently inhibits RSL3-induced ferroptosis in H9c2 cells with an EC50 of 93 nM[1].
Ferroptosis-IN-26 potently inhibits RSL3-induced ferroptosis in SK-HEP-1 cells with an EC50 of 102 nM[1].
Ferroptosis-IN-26 potently inhibits Erastin (HY-15763)-induced ferroptosis in HT-1080 cells with an EC50 of 0.27 μM[1].
Ferroptosis-IN-26 potently inhibits FIN56 (HY-103087)-induced ferroptosis in HT-1080 cells with an EC50 of 0.32 μM[1].
Ferroptosis-IN-26 (1 μM) suppresses RSL3-induced lipid ROS accumulation in 786-O and H9c2 cells[1].
Ferroptosis-IN-26 (1 μM) suppresses Erastin- and FIN56-induced lipid ROS accumulation in HT-1080 cells[1].
Ferroptosis-IN-26 (1 μM; 24 h) does not protect SK-HEP-1 or 786-O cells against STS-induced apoptosis[1].
Ferroptosis-IN-26 (1 μM; 24 h) does not protect SK-HEP-1 or 786-O cells against H2O2-induced necrosis[1].
Ferroptosis-IN-26 (up to 1.5 μM; 24 h) has low inherent cytotoxicity in HEK293T cells, with a CC50 greater than 20 μM[1].
Ferroptosis-IN-26 (1-2 μM; 0-180 min) does not inhibit AAPH (HY-Y0525)-induced lipid peroxidation in EggPC liposomes[1].
Ferroptosis-IN-26 (50 μM) does not exhibit DPPH radical scavenging activity[1].
Ferroptosis-IN-26 does not alter cellular glutathione levels in cells treated with Erastin[1].
Ferroptosis-IN-26 does not alter cellular total free thiol levels in cells treated with Erastin[1].
Ferroptosis-IN-26 (0.5-10 μM) does not alter the expression of ferroptosis-associated proteins in cells[1].
Ferroptosis-IN-26 inhibits RSL3-induced ferroptosis in SK-HEP-1 and 786-O cells independently of the FSP1/CoQ10 system[1].
Ferroptosis-IN-26 inhibits RSL3-induced ferroptosis in GPX4-knockout HT-1080 cells, demonstrating activity independent of GPX4 function[1].
Ferroptosis-IN-26 (3 μM; 72 h) increases cellular levels of MUFA-enriched phosphatidylcholine species in 786-O cells[1].
The antiferroptotic activity of Ferroptosis-IN-26 in SCD1-knockout 786-O and HT-1080 cells is independent of SCD1-mediated MUFA generation[1].

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

Cell Viability Assay[1]

Cell Line: SK-HEP-1 cells; 786-O cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Did not protect SK-HEP-1 or 786-O cells against STS-induced apoptosis.

Cell Viability Assay[1]

Cell Line: SK-HEP-1 cells; 786-O cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Did not protect SK-HEP-1 or 786-O cells against H2O2-induced necrosis.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUClast AUCINF_obs MRTINF_obs F ClF_obs Vss_obs
Rat[1] 5 mg/kg i.v. 2.718 h / / 2034.418 ng·h/mL 2054.383 ng·h/mL 1.577 h / 40.779 mL/min/kg 3817.128 mL/kg
Rat[1] 10 mg/kg p.o. 4.92 h 1.0 h 75.667 ng/mL 210.351 ng·h/mL 221.607 ng·h/mL 4.973 h 5.2 % / /
In Vivo

Ferroptosis-IN-26 (Compound 4g) (10 mg/kg) protects against hepatic ischemia-reperfusion injury in mice by mitigating ferroptosis-related hepatocellular damage, lipid peroxidation, and iron accumulation[1].
Ferroptosis-IN-26 (5-10 mg/kg) ameliorates ConA (HY-P2149)-induced acute liver injury in mice by suppressing ferroptosis and hepatocellular damage[1].
Ferroptosis-IN-26 (5 mg/kg) ameliorates APAP (HY-66005)-induced acute liver injury in C57 mice by improving liver function and reducing hepatocellular damage[1].

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

Animal Model: C57BL/6 mice (male; eight weeks old; intravenously injected with 15 mg/kg ConA to establish an acute liver injury model)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: i.p.; 2 doses administered 24 h apart
Result: Significantly alleviated hepatocellular lesions.
Markedly reduced serum levels of the liver injury markers ALT and AST.
Substantially decreased 4-HNE adducts.
Significantly reduced serum MDA levels.
Downregulated the mRNA expression of the ferroptosis-associated gene Ptgs2 in mice livers.
Animal Model: C57BL/6 mice (male; six weeks old; 18-22 g; intraperitoneally injected with 400 mg/kg APAP to establish an acute liver injury model)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: i.p.; 2 doses administered 24 h apart
Result: Markedly reduced serum levels of the liver injury markers ALT and AST.
Animal Model: C57BL/6 mice (male; eight weeks old; hepatic ischemia-reperfusion injury)[1]
Dosage: 10 mg/kg
Administration: i.p.; 2 doses at 36 h and again
at 12 h prior to surgery
Result: Markedly ameliorated extensive ischemic areas and inflammatory infiltration.
Significantly attenuated the HIRI-induced elevation in serum ALT and AST levels.
Significantly reduced serum MDA levels.
Molecular Weight

364.40

Formula

C24H16N2O2

SMILES

CC1=CC2=C(C=C1O)OC3=NC4=C(C(C=CC=C5)=C5N4)C(C6=CC=CC=C6)=C32

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    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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Product Name:
Ferroptosis-IN-26
Cat. No.:
HY-183589
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