Cat. No.: HY-112675

4-Octyl itaconate

(Synonyms: 4-OI)

94 Cited Publications

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Based on 94 publication(s) in Google Scholar

4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1.

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Pureté: 99.92%
CAS No.: 3133-16-2
Formule: C₁₃H₂₂O₄
Masse moléculaire:242.31

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

4-Octyl itaconate Chemical Structure

CAS No.: 3133-16-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Publications (94)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
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Activité biologique

Description

4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1^[1].

IC₅₀ & Target

Nrf2^[1]

In Vivo

4-Octyl Itaconate (OI) is a cell-permeable itaconate derivative. 4-Octyl Itaconate is protective against lipopolysaccharide-induced lethality in vivo and decreases cytokine production^[1].

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

Chemical Information

CAS No. 3133-16-2
Appearance Solid
Masse moléculaire 242.31
Formule C₁₃H₂₂O₄
Color White to off-white
SMILES

O=C(OCCCCCCCC)CC(C(O)=O)=C
Synonyms

4-OI
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (94)

All 2D/3D Cell Culture and DifferentiationIn Vivo Efficacy StudyHistological Imaging/StainingBio/Physico-chemical AssayOthersCell Migration/Invasion AssayELISART-PCRCell Proliferation/Viability AssayIFFlow CytometryIPWB

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Journal Impact Factor

Cell Metab

Itaconate transporter SLC13A3 confers immunotherapy resistance via alkylation-mediated stabilization of PD-L1. [Abstract]

2025 Feb 4;37(2):514-526.e5. PMID: 39809284

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2025 Feb 4;37(2):514-526.e5. [Abstract]

Pathway enrichment analysis and enrichment scores of immune-related pathways in murine carcinoma Renca cells after OI (4-Octyl itaconate; 50 μM; 12 h) treatment. Multiple immune-response-related pathways were downregulated after OI treatment.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2025 Feb 4;37(2):514-526.e5. [Abstract]

IFN-sensitive gene mRNA expression in Renca cells after OI (4-Octyl itaconate, 4-OI; 50 μM; 12 h) treatment was determined by real-time qPCR. OI decreased the expression of multiple IFN-sensitive and antigen-presentation genes.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2025 Feb 4;37(2):514-526.e5. [Abstract]

PD-L1 protein levels in 786-O, A549, and Renca cells treated with 4-OI (4-Octyl itaconate; 50 μM; 12 h) were analyzed by immunoblotting.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2025 Feb 4;37(2):514-526.e5. [Abstract]

Immunofluorescence analyses of PD-L1 in human 786-O and A549 cells with or without 4-OI (4-Octyl itaconate; 50 μM; 12 h) treatment.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2025 Feb 4;37(2):514-526.e5. [Abstract]

Deubiquitination and deneddylation related proteins enriched in the HA-PD-L1 precipitates upon 4-OI (4-Octyl itaconate; 50 μM) treatment for 12 h. PD-L1 modified by 4-OI showed stronger affinity for deubiquitinating enzymes including USP22, USP5, and USP7.
Cell Metab

2019 Aug.
Cell Mol Immunol

The alkylation of AIM2 by itaconate mediates macrophage PANoptosis during sepsis. [Abstract]

2026 Jun;23(6):619-634. PMID: 42120931

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2026 Jun;23(6):619-634. [Abstract]

Kaplan-Meier survival curves of WT and Acod1^−/− mice over 7 days following middle-grade sepsis. Exogenous 4-OI (4-Octyl itaconate; 50 mg/kg; i.p.; at 2, 24, 48, and 72 h post-CLP) administration drastically curtailed the survival of Acod1^−/− mice and further exacerbated mortality in WT septic mice.
Bone Res

Inflammatory macrophage-derived itaconate inhibits DNA demethylase TET2 to prevent excessive osteoclast activation in rheumatoid arthritis. [Abstract]

2025 Jun 11;13(1):60. PMID: 40500265

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 11;13(1):60. [Abstract]

Representative TRAP staining images and quantification of TRAP⁺ osteoclasts of mature osteoclasts at day 5 from different treatments. OI (4-Octyl itaconate; 12.5-50 μM; 5 days) significantly inhibited osteoclast differentiation.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 11;13(1):60. [Abstract]

Representative images of pit formation assay and quantification of bone resorption area of Irg1^+/+ and Irg1^−/− after 7 days of osteoclast induction with or without the addition of 50 μmol/L OI (4-Octyl itaconate; 7 days). OI reduced bone resorption activity in both genotypes.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 11;13(1):60. [Abstract]

DNA dot blot analysis of 5hmC levels in osteoclasts treated with OI (4-Octyl itaconate; 50 μmol/L) during differentiation on days 1 and 3. OI reduced genomic DNA 5hmC levels in osteoclasts.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 11;13(1):60. [Abstract]

Expression levels of Acp5, Ctsk, and Mmp9 protein during osteoclast differentiation on days 0, 1, 3, and 5 with or without OI (4-Octyl itaconate; 50 μmol/L). OI reduced Acp5, Ctsk, and Mmp9 protein levels.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 11;13(1):60. [Abstract]

Promoter demethylation Status of Acp5, Ctsk, and Mmp9 following three days of osteoclastogenesis in the presence or absence of OI (4-Octyl itaconate; 50 μM; 3 days). OI robustly suppressed DNA demethylation at the promoter regions of Acp5, Ctsk, and Mmp9 on the third day of osteoclast differentiation.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 11;13(1):60. [Abstract]

CCK-8 assay of BMMs cell viability at 0, 24, 48, 72, and 96 hours exposed to different concentrations of OI (4-Octyl itaconate; 3.125-50 μM). OI did not significantly affect BMM viability across the tested concentrations and time points.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 11;13(1):60. [Abstract]

Measurement of CD86 and CD206 expression in human RA-MDMs treated with or without OI (4-Octyl itaconate; 100 μmol/L; 24 h). OI-treated macrophages exhibited a more reparative phenotype.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 11;13(1):60. [Abstract]

Expression of NOS2, IL1B, CD163 and CD206 in human RA-MDMs treated with or without OI (4-Octyl itaconate; 100 μmol/L; 12 h). OI-treated macrophages exhibited a more reparative phenotype.
Nat Commun

Metabolic Reprogramming via ACOD1 depletion enhances function of human induced pluripotent stem cell-derived CAR-macrophages in solid tumors. [Abstract]

2023 Sep 18;14(1):5778. PMID: 37723178
Int J Oral Sci

Four-Octyl itaconate ameliorates periodontal destruction via Nrf2-dependent antioxidant system. [Abstract]

2022 May 31;14(1):27. PMID: 35637195

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2022 May 31;14(1):27. [Abstract]

Hematoxylin and eosin (H&E) staining indicated 4-octyl itaconate (4-OI) (50 mg/kg; injected locally; daily for 14 days ) could play a pivotal role in decreasing alveolar bone loss in experimental periodontitis models.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2022 May 31;14(1):27. [Abstract]

4-octyl itaconate (4-OI; 200 μM) induces a shift in polarization phenotype of macrophages in vitro. Expression of M1 and M2-related genes in RAW 264.7 using qRT-PCR (The M1-related IL-1β, IL-6, CCL2, iNOS, CD86, and the M2-related TGF-β, Arg-1 and CD206).

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2022 May 31;14(1):27. [Abstract]

4-octyl itaconate (4-OI; 200 μM) induces a shift in polarization phenotype of macrophages in vitro. Micrographs showing staining of iNOS, CD86 and CD206 obtained using confocal laser scanning microscopy.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2022 May 31;14(1):27. [Abstract]

The role of Nrf2 exerted in the protection of 4-octyl itaconate (4-OI; 200 μM) against periodontal inflammation. a The Nrf2 protein expression in nuclei fraction lysates quantified by Western blotting. The expression of Nrf2 downstream ARE-dependent proteins in RAW264.7 measured by Western blotting.
Exp Mol Med

Identification of a metabolic-immune crosstalk in Still's disease: monocyte/macrophage-derived immunometabolite itaconate dictates hepatic immunopathology via the CXCL10-CD8 T cell axis. [Abstract]

2026 Jun;58(6):1927-1939. PMID: 42249091

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2026 Jun;58(6):1927-1939. [Abstract]

Il1b and Il6 mRNA in CpG-treated (1 μM, 3 h) BMDMs with 2 h pretreatment of 100 μM 4-OI (4-Octyl itaconate; 100 μM). 4-OI suppressed CpG-induced Il1b and Il6 expression.
ACS Nano

On-Demand Collaborative Delivery for Remodeling the Senescent Microenvironment in Intervertebral Disc Degeneration. [Abstract]

2025 Oct 28. PMID: 41147252
J Adv Res

Nrf2 deficiency in myeloid cells accelerates atherosclerosis by promoting the inflammatory response and impairing efferocytosis. [Abstract]

2026 Jan 2:S2090-1232(26)00005-6. PMID: 41485574
Redox Biol

ACOD1-itaconate in macrophage attenuates oxidative stress and inflammation in benign airway stenosis by upregulating and transferring FTH1. [Abstract]

2026 May:92:104133. PMID: 41865719

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 May:92:104133. [Abstract]

Representative images of Masson staining and relative collagen content in control group, BAS group and BAS+4-OI (4-Octyl itaconate; 25 mg/kg; i.p.; 12 h before modeling, within 5 min after injury establishment, and on days 2, 4, and 6 after modeling) group at day 7 after modeling. Elevated collagen deposition in BAS mice was significantly reduced by 4-OI.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 May:92:104133. [Abstract]

Representative tracheal immunofluorescence images of IL6 (red), IL1β (green) in control group, BAS group and BAS group treated with 4-OI (4-Octyl itaconate; 25 mg/kg; i.p.; 12 h before modeling and within 5 min after injury establishment) at day1 after modeling. 4-OI reduced IL-6 and IL-1β levels.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 May:92:104133. [Abstract]

qPCR analysis demonstrated that treatment with 4-OI (4-Octyl itaconate; 125 μM; 24 h) suppressed LPS-induced mRNA expression of IL6 and IL1β in macrophages compared with the LPS-stimulated vehicle control.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 May:92:104133. [Abstract]

FTH1 secretion in macrophage supernatants was measured by ELISA after 4-OI treatment (4-Octyl itaconate; 125 μM; 24 h). 4-OI alone did not alter basal FTH1 secretion but significantly increased FTH1 release under LPS-induced inflammatory conditions.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 May:92:104133. [Abstract]

Western blot analysis of FTH1 protein levels in macrophages after 4-OI (4-Octyl itaconate; 125 μM; 24 h) treatment. 4-OI rescued LPS-induced FTH1 downregulation.
Redox Biol

Stromal cell-derived itaconate promotes endometriosis via macrophage NRF2 and lysosomal pH modulation. [Abstract]

2026 May:92:104101. PMID: 41780193

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 May:92:104101. [Abstract]

Western blot analysis and quantification of NRF2 protein levels in bone marrow-derived macrophages (BMDMs) pretreated with LPS (100 ng/mL), 4-octyl itaconate (4-OI; 250 μM), or both for 12 h. 4-OI markedly increased NRF2 protein expression.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 May:92:104101. [Abstract]

mESCs were co-cultured with BMDMs for 12 hours, with or without 4-OI (4-Octyl itaconate; 250 μM). mRNA levels of Il1b, Il6, Tnfa, and Nos2 were determined by qRT-PCR (n = 3 / group). 4-OI suppressed macrophage pro-inflammatory activation.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 May:92:104101. [Abstract]

Representative dot plots and histograms showing phagocytosis of PKH67-labeled mESCs by F4/80⁺ macrophages after LPS or LPS + 4-OI (4-Octyl itaconate; 250 μM; 10 h) treatment.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 May:92:104101. [Abstract]

Representative images and quantification of migrated mESCs in a transwell assay co-cultured with LPS- or LPS + 4-OI-treated (4-Octyl itaconate; 250 μM; 10 h) BMDMs.
Redox Biol

Unveiling a novel function of Aconitase-2: attenuating lung ischemia-reperfusion injury via inhibition of pulmonary endothelial apoptosis. [Abstract]

2026 Mar:90:104016. PMID: 41637882

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104016. [Abstract]

Quantitative assessment of lung injury via histopathological scoring. 4-OI (4-Octyl itaconate; 25 mg/kg/day; i.p.) reduced the TA-associated increase in lung injury scores.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104016. [Abstract]

Representative H&E-stained lung sections. 4-OI (4-Octyl itaconate; 25 mg/kg/day; i.p.) significantly attenuated TA-induced alveolar wall thickening.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104016. [Abstract]

Metabolic ratios of NAD⁺/NADH and ATP/ADP. 4-OI (4-Octyl itaconate; 25 mg/kg/day; i.p.) reversed the TA-induced reductions in NAD⁺/NADH and ATP/ADP ratios.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104016. [Abstract]

Apoptosis-related protein contents (cleaved caspase-3, Bcl-2, and BAX) analyzed by western blot with semi-quantitative analysis. 4-OI (4-Octyl itaconate; 25 mg/kg/day; i.p.) exerted anti-apoptotic effects by upregulating Bcl-2 and downregulating cleaved caspase-3 and BAX contents.
Mol Cell

Itaconate is a lysosomal inducer that promotes antibacterial innate immunity. [Abstract]

2022 Aug 4;82(15):2844-2857.e10. PMID: 35662396
J Nanobiotechnology

Biomimetic hybrid nanoparticles for dual regulation of macrophage pyroptosis and metabolism in rheumatoid arthritis. [Abstract]

2026 May 8;24(1):652. PMID: 42104436

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2026 May 8;24(1):652. [Abstract]

CCK-8 assay of J774A.1 cells after treatment with 4-OI (4-Octyl itaconate; 50-600 μM; 48 h). CCK-8 assays indicated that the safe concentration of free 4-OI in J774A.1 cells was below 200 µM.
J Nanobiotechnology

Bioinspired nanovesicles released from injectable hydrogels facilitate diabetic wound healing by regulating macrophage polarization and endothelial cell dysfunction. [Abstract]

2023 Oct 3;21(1):358. PMID: 37789401
Genes Dis

Protective effects of IRG1/itaconate on acute colitis through the inhibition of gasdermins-mediated pyroptosis and inflammation response. [Abstract]

2022 Jun 20;10(4):1552-1563. PMID: 37397544
Adv Sci (Weinh)

4-Octyl Itaconate Alleviates Myocardial Ischemia-Reperfusion Injury Through Promoting Angiogenesis via ERK Signaling Activation. [Abstract]

2025 Mar;12(10):e2411554. PMID: 39836624
Cell Death Differ

Itaconate protects ferroptotic neurons by alkylating GPx4 post stroke. [Abstract]

2024 Aug;31(8):983-998. PMID: 38719928
Mol Biomed

Neutrophil Irg1/itaconate axis protects against experimental colitis by suppressing local inflammation and maintaining hematopoietic homeostasis. [Abstract]

2025 Dec 19;6(1):143. PMID: 41417165
Cell Death Dis

Immune-responsive gene 1/itaconate activates nuclear factor erythroid 2-related factor 2 in microglia to protect against spinal cord injury in mice. [Abstract]

2022 Feb 10;13(2):140. PMID: 35145070

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Feb 10;13(2):140. [Abstract]

Cell Counting Kit-8 (CCK-8) results for microglia treated with different concentrations of 4-Octyl Itaconate (4-OI) for 24 and 48 h.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Feb 10;13(2):140. [Abstract]

Evaluated the effect of 4-Octyl Itaconate (4-OI; 20-80 μM) on the LPS-induced inflammation model. The mRNA expression of iNOS, COX2 and IL-6 are measured by qRT-PCR.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Feb 10;13(2):140. [Abstract]

Evaluated the effect of 4-Octyl Itaconate (4-OI; 20-80 μM) on the LPS-induced inflammation model. The protein expression of iNOS, COX2 and IL-6 are measured by western blot.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Feb 10;13(2):140. [Abstract]

After 48 h of co-cultivation with 4-Octyl Itaconate (4-OI; 80 μM)-treated microglia, the proportion of apoptotic PC12 cells decreased significantly, the expression of Cleave-caspase3 decreased, and the expression of Bcl2 increased.
Int J Biol Sci

4-Octyl itaconate regulates immune balance by activating Nrf2 and negatively regulating PD-L1 in a mouse model of sepsis. [Abstract]

2022 Oct 24;18(16):6189-6209. PMID: 36439878

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2022 Oct 24;18(16):6189-6209. [Abstract]

Western blotting confirmes that TNF-α, IL-1β, and IFN-γ expression are significantly higher in RAW264.7 cells treated with LPS and are significantly inhibited by OI (4-Octyl Itaconate) (62.5, 125 µM; 12 h).
Cell Commun Signal

IRG1/itaconate enhances efferocytosis by activating Nrf2-TIM4 signaling pathway to alleviate con A induced autoimmune liver injury. [Abstract]

2025 Feb 5;23(1):63. PMID: 39910615
J Neuroinflammation

Accumulated BCAAs and BCKAs contribute to the HFD-induced deterioration of Alzheimer's disease via a dysfunctional TREM2-related reduction in microglial β-amyloid clearance. [Abstract]

2024 Dec 23;21(1):327. PMID: 39716292
Phytomedicine

Schisandrin B alleviates liver allograft rejection by stabilizing ACOD1 in Kupffer cells to potentiate itaconate-NRF2-mediated suppression of CD8+ T cell chemotaxis. [Abstract]

2026 May:154:158031. PMID: 41795300
Cell Death Discov

Itaconate inhibits ferroptosis of macrophage via Nrf2 pathways against sepsis-induced acute lung injury. [Abstract]

2022 Feb 2;8(1):43. PMID: 35110526
Proc Natl Acad Sci U S A

The IRG1-itaconate axis protects from cholesterol-induced inflammation and atherosclerosis. [Abstract]

2024 Apr 9;121(15):e2400675121. PMID: 38564634
Apoptosis

Pharmacological inhibition of STING-mediated GPX4 autophagic degradation by 4-octyl itaconate ameliorates sepsis-induced acute kidney injury. [Abstract]

2025 Jun;30(5-6):1410-1423. PMID: 40119983
Apoptosis

Itaconate promotes mitophagy to inhibit neuronal ferroptosis after subarachnoid hemorrhage. [Abstract]

2025 Apr;30(3-4):991-1004. PMID: 39924585
Apoptosis

IRG1/Itaconate inhibits proliferation and promotes apoptosis of CD69+CD103+CD8+ tissue-resident memory T cells in autoimmune hepatitis by regulating the JAK3/STAT3/P53 signalling pathway. [Abstract]

2024 Oct;29(9-10):1738-1756. PMID: 38641760
BMC Med

Dimethyl itaconate suppresses dendritic cell and CD8+ T cell responses to halt vitiligo. [Abstract]

2025 Dec 29;23(1):698. PMID: 41466279
Regen Biomater

Fabrication of a 3D bioprinting model for posterior capsule opacification using GelMA and PLMA hydrogel-coated resin. [Abstract]

2024 Mar 1:11:rbae020. PMID: 38529352
Mol Med

CpG-oligodeoxynucleotides challenged macrophages ameliorate acetaminophen induced liver injury by activating TLR9/IRG1/itaconate metabolic pathway. [Abstract]

2025 Aug 25;31(1):282. PMID: 40855408
Free Radic Biol Med

4-Octyl itaconate suppresses the osteogenic response in aortic valvular interstitial cells via the Nrf2 pathway and alleviates aortic stenosis in mice with direct wire injury. [Abstract]

2022 Aug 1;188:404-418. PMID: 35787451

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Aug 1;188:404-418. [Abstract]

CCK-8 assay of the viability of valve interstitial cells treated with different concentrations of 4-Octyl Itaconate (OI) for 24 h.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Aug 1;188:404-418. [Abstract]

Representative images showing immunofluorescent staining of Nrf2 (red) after valve interstitial cells are treated with 40 μM 4-Octyl Itaconate (OI) for 2 h.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Aug 1;188:404-418. [Abstract]

Relative quantification of the mRNA expression of Nrf2, Hmox1 and NQO1 after valve interstitial cells are treated with different concentrations of 4-Octyl Itaconate (OI) for 4 h.

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Aug 1;188:404-418. [Abstract]

Representative Western blot images and quantification of Hmox1 and NQO1 protein expression after valve interstitial cells are treated with different concentrations of 4-Octyl Itaconate (OI) for 24 h.
Free Radic Biol Med

Immune-responsive gene 1 protects against liver injury caused by concanavalin A via the activation Nrf2/HO-1 pathway and inhibition of ROS activation pathways. [Abstract]

2022 Mar:182:108-118. PMID: 35231555
Clin Transl Med

ACOD1, rather than itaconate, facilitates p62-mediated activation of Nrf2 in microglia post spinal cord contusion. [Abstract]

2024 Apr;14(4):e1661. PMID: 38644791
Cell Rep

4-octyl itaconate inhibits cytokine-mediated inflammation via alkylation of TYK2 and JAK1. [Abstract]

2026 Mar 30;45(4):117179. PMID: 41915469
Cell Rep

4-octyl itaconate as a metabolite derivative inhibits inflammation via alkylation of STING. [Abstract]

2023 Feb 28;42(3):112145. PMID: 36862550

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Feb 28;42(3):112145. [Abstract]

4-Octyl Itaconate (4-OI; 250 µM; 2 h) significantly inhibits the phosphorylation of STING and the activation of downstream signaling molecules in RAW264.7 macrophages.
Biochem Pharmacol

ACOD1/Itaconate regulates trophoblast function through the PI3K/Akt/FOLR1 axis to participate in the pathogenesis of recurrent spontaneous abortion. [Abstract]

2025 Dec;242(Pt 3):117405. PMID: 41047036
Biochem Pharmacol

Macrophage scavenger receptor A1 antagonizes abdominal aortic aneurysm via upregulating IRG1. [Abstract]

2023 Jul:213:115631. PMID: 37257722
Biochem Pharmacol

Itaconate alleviates β2-microglobulin-induced cognitive impairment by enhancing the hippocampal amino-β-carboxymuconate-semialdehyde-decarboxylase/picolinic acid pathway. [Abstract]

2022 Aug:202:115137. PMID: 35700758
Biochem Pharmacol

Itaconate attenuates osteoarthritis by inhibiting STING/NF-κB axis in chondrocytes and promoting M2 polarization in macrophages. [Abstract]

2022 Apr:198:114935. PMID: 35104478
Inflammopharmacology

4-Octyl itaconate alleviates dextran sulfate sodium-induced ulcerative colitis in mice via activating the KEAP1-NRF2 pathway. [Abstract]

2024 Aug;32(4):2555-2574. PMID: 38767761
J Cell Biol

Irg1l regulates neuromast size via metabolic reprogramming to promote supporting cell proliferation. [Abstract]

2025 Dec 1;224(12):e202501122. PMID: 41147954
Biomater Sci

Injectable hydrogel loaded with 4-octyl itaconate enhances cartilage regeneration by regulating macrophage polarization. [Abstract]

2023 Mar 28;11(7):2445-2460. PMID: 36757828
Cells

Ameliorative Effect of Itaconic Acid/IRG1 Against Endoplasmic Reticulum Stress-Induced Necroptosis in Granulosa Cells via PERK-ATF4-AChE Pathway in Bovine. [Abstract]

2025 Mar 12;14(6):419. PMID: 40136668
Commun Biol

Protective role of aconitate decarboxylase 1 in neuroinflammation-induced dysfunctions of the paraventricular thalamus and sleepiness. [Abstract]

2024 Nov 10;7(1):1484. PMID: 39523388
Commun Biol

Four-octyl itaconate improves osteoarthritis by enhancing autophagy in chondrocytes via PI3K/AKT/mTOR signalling pathway inhibition. [Abstract]

2022 Jun 29;5(1):641. PMID: 35768581
Eur J Pharmacol

4-Octyl itaconate inhibits vascular calcification partially via modulation of HMOX-1 signaling. [Abstract]

2024 Dec 15:985:177122. PMID: 39532225
Int Immunopharmacol

IRG1/Itaconate inhibits hepatic stellate cells ferroptosis and attenuates TAA-induced liver fibrosis by regulating SLC39A14 expression. [Abstract]

2025 Jan 27:146:113945. PMID: 39724735
Int Immunopharmacol

IRG1/itaconate alleviates acute liver injury in septic mice by suppressing NLRP3 expression and its mediated macrophage pyroptosis via regulation of the Nrf2 pathway. [Abstract]

2024 Jun 30:135:112277. PMID: 38788445
Int Immunopharmacol

4-Octyl itaconate inhibits inflammation to attenuate psoriasis as an agonist of oxeiptosis. [Abstract]

2023 Sep 21;124(Pt B):110915. PMID: 37741130
Int J Mol Sci

Aconitate Decarboxylase 1 Deficiency Exacerbates Mouse Colitis Induced by Dextran Sodium Sulfate. [Abstract]

2022 Apr 15;23(8):4392. PMID: 35457208
Inflammation

4-Octyl Itaconate Attenuates Neuroinflammation in Experimental Autoimmune Encephalomyelitis Via Regulating Microglia. [Abstract]

2025 Feb;48(1):151-164. PMID: 38761250
Front Pharmacol

4-OI Attenuates Carbon Tetrachloride-Induced Hepatic Injury via Regulating Oxidative Stress and the Inflammatory Response. [Abstract]

2021 May 25:12:651444. PMID: 34113251

4-Octyl itaconate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 May 25:12:651444. [Abstract]

Nrf2 knockdown attenuates the protective effect of 4-Octyl Itaconate (OI) in CCl4-treated NCTC 1469 cells.
Front Chem

The Emerging Application of Itaconate: Promising Molecular Targets and Therapeutic Opportunities. [Abstract]

2021 May 12;9:669308. PMID: 34055739
Biochim Biophys Acta Mol Basis Dis

Nrf2 protects against oxidative damage induced by hemoglobin in the liver of grass carp (Ctenopharyngodon idella). [Abstract]

2024 Nov 29;1871(3):167600. PMID: 39615659
Biochim Biophys Acta Mol Basis Dis

Immune response gene 1 deficiency aggravates high fat diet-induced nonalcoholic fatty liver disease via promotion of redox-sensitive AKT suppression. [Abstract]

2023 Apr;1869(4):166656. PMID: 36706797
Sci Rep

Protective role of IRG1/itaconate in acute myocardial injury: association with NLRP3 inflammasome and oxidative stress. [Abstract]

2026 Mar 13;16(1):13365. PMID: 41826607
Sci Rep

Pomolic acid alleviates CCl4‑induced liver fibrosis in mice by suppressing β-arrestin 2-mediated pro-fibrotic macrophage polarization. [Abstract]

2026 Mar 31. PMID: 41917130
Sci Rep

4-Octyl itaconate alleviates sepsis-induced liver injury by regulating ferroptosis via the OTUB1/TRAF3 axis. [Abstract]

2026 Feb 10;16(1):8201. PMID: 41667684
Mater Today Commun

2025 Feb.
PLoS Pathog

Pharmacological inhibition of bromodomain and extra-terminal proteins induces an NRF-2-mediated antiviral state that is subverted by SARS-CoV-2 infection. [Abstract]

2023 Sep 25;19(9):e1011657. PMID: 37747932
Sci Rep

Nrf2 inhibition increases sensitivity to chemotherapy of colorectal cancer by promoting ferroptosis and pyroptosis. [Abstract]

2023 Sep 1;13(1):14359. PMID: 37658132
Mediators Inflamm

Hepatoprotective Role of 4-Octyl Itaconate in Concanavalin A-Induced Autoimmune Hepatitis. [Abstract]

2022 Mar 11:2022:5766434. PMID: 35310452
J Pharm Investig

2025 Jun 25.
J Cell Mol Med

4-octyl itaconate alleviates cisplatin-induced ferroptosis possibly via activating the NRF2/HO-1 signalling pathway. [Abstract]

2024 Apr;28(7):e18207. PMID: 38506087
Adv Ophthalmol Pract Res

2026 Jan 14.
FASEB J

Octyl itaconate inhibits osteoclastogenesis by suppressing Hrd1 and activating Nrf2 signaling. [Abstract]

2019 Nov;33(11):12929-12940. PMID: 31490085
Med Gas Res

Mechanism by which hydrogen-rich water mitigates exercise-induced fatigue: activation of the immunoresponsive gene 1-itaconate/nuclear factor erythroid 2-related factor 2/heme oxygenase-1 pathway. [Abstract]

2026 Mar 1;16(1):26-32. PMID: 40580185
J Funct Foods

2023 Mar.
Ren Fail

4-Octyl itaconate attenuates renal tubular injury in db/db mice by activating Nrf2 and promoting PGC-1α-mediated mitochondrial biogenesis. [Abstract]

2024 Dec;46(2):2403653. PMID: 39291665
Exp Biol Med

4-Octyl itaconate alleviates renal ischemia reperfusion injury by ameliorating endoplasmic reticulum stress via Nrf2 pathway. [Abstract]

2023 Dec;248(23):2408-2420. PMID: 38158612
Arch Biochem Biophys

RNA-seq transcriptomic analysis of 4-octyl itaconate repressing myogenic differentiation. [Abstract]

2022 Nov 30:731:109420. PMID: 36183843
Mol Biol Rep

MPP+ disorders Irg1-Itaconate axis to promote M1 polarization of microglia by activating succinate dehydrogenase. [Abstract]

2025 Nov 24;53(1):115. PMID: 41284105
IUBMB Life

Contrast-Induced Acute Kidney Injury is Modulated by Circadian CLOCK/NRF2 Pathway. [Abstract]

2025 May;77(5):e70022. PMID: 40391788
PLoS One

Itaconic acid inhibits nontuberculous mycobacterial growth in pH dependent manner while 4-octyl-itaconic acid enhances THP-1 clearance of nontuberculous mycobacteria in vitro. [Abstract]

2024 May 10;19(5):e0303516. PMID: 38728330
Virology

Itaconate derivative 4-OI inhibits PRRSV proliferation and associated inflammatory response. [Abstract]

2022 Dec:577:84-90. PMID: 36323047
Biochem Biophys Res Commun

Protective effects of 4-octyl itaconate against inflammatory response in angiotensin II-induced oxidative stress in human primary retinal pigment epithelium. [Abstract]

2021 Jun 11:557:77-84. PMID: 33862463
J Mol Neurosci

The Prevention and Reversal of a Phenytoin-Resistant Model by N-acetylcysteine Therapy Involves the Nrf2/P-Glycoprotein Pathway at the Blood-Brain Barrier. [Abstract]

2022 Oct;72(10):2125-2135. PMID: 36028602
Exp Ther Med

4-Octyl itaconate (4-OI) attenuates lipopolysaccharide-induced acute lung injury by suppressing PI3K/Akt/NF-κB signaling pathways in mice. [Abstract]

2021 Feb;21(2):141. PMID: 33456508
Inhal Toxicol

4-OI improves mitochondria-associated endoplasmic reticulum membrane dysfunction by regulating MFN2 through Nrf2 transcription and alleviates airway inflammation in asthma exposed to PM2.5 early in life. [Abstract]

2026 May;38(5):252-267. PMID: 41902706
Naturwissenschaften

Gamma-aminobutyric acid attenuates cortisol-induced damage in human colorectal adenocarcinoma cells via Nrf2 signaling. [Abstract]

2025 Oct 20;112(6):82. PMID: 41114738
J Physiol Investig

Itaconate Attenuates Homocysteine-induced Nod-like Receptor Family Protein 3 Inflammasome-mediated Pyroptosis in Hippocampal Neurons: Involvement of Inhibiting Succinate Dehydrogenase Complex Subunit A Level. [Abstract]

2025 Jul 4. PMID: 40616278
Res Sq

2026 Jun 5.
SSRN

2026 May 15.
bioRxiv

2026 Mar 29.
SSRN

2025 Jul 29.
bioRxiv

2024 Feb 21.
Biomed Pharmacother

4-Octyl itaconate inhibits aerobic glycolysis by targeting GAPDH to promote cuproptosis in colorectal cancer. [Abstract]

2023 Mar:159:114301. PMID: 36706634
Research Square Print

2023 Jan 24.
Research Square Print

November 29th, 2022.
Oxid Med Cell Longev

Four-Octyl Itaconate Attenuates UVB-Induced Melanocytes and Keratinocytes Apoptosis by Nrf2 Activation-Dependent ROS Inhibition. [Abstract]

2022 Mar 11:2022:9897442. PMID: 35308171
Oxid Med Cell Longev

Protective Role of 4-Octyl Itaconate in Murine LPS/D-GalN-Induced Acute Liver Failure via Inhibiting Inflammation, Oxidative Stress, and Apoptosis. [Abstract]

2021 Aug 17:2021:9932099. PMID: 34457120
Ann Transl Med

Itaconate ameliorates methicillin-resistant Staphylococcus aureus-induced acute lung injury through the Nrf2/ARE pathway. [Abstract]

2021 Apr;9(8):712. PMID: 33987410

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (412.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.1269 mL

20.6347 mL

41.2694 mL

5 mM

0.8254 mL

4.1269 mL

8.2539 mL

10 mM

0.4127 mL

2.0635 mL

4.1269 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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