2. Immunology/Inflammation Apoptosis
  3. NOD-like Receptor (NLR) Caspase Interleukin Related
  4. 1,2,4-Trimethoxybenzene

1,2,4-Trimethoxybenzene is an orally active NLRP3 selective inhibitor. 1,2,4-Trimethoxybenzene can markedly suppress Nigericin (HY-127019) or ATP (HY-B2176)-induced NLRP3 inflammasome activation, thus decreasing caspase-1 activation and IL-1β secretion. 1,2,4-Trimethoxybenzene specifically inhibits the activation of NLRP3 inflammasome without affecting absent in melanoma 2 (AIM2) inflammasome activation. 1,2,4-Trimethoxybenzene inhibits oligomerization of the apoptosis-associated speck-like protein containing a CARD (ASC) and protein-protein interaction between NLRP3 and ASC, thus blocking NLRP3 inflammasome assembly. 1,2,4-Trimethoxybenzene can be used for the study of experimental autoimmune encephalomyelitis (EAE), multiple sclerosis, and type 2 diabetes.

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1,2,4-Trimethoxybenzene

1,2,4-Trimethoxybenzene Chemical Structure

CAS No. : 135-77-3

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1,2,4-Trimethoxybenzene Related Antibodies

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NLRP3 NLRP1 NOD1 NOD2

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

1,2,4-Trimethoxybenzene is an orally active NLRP3 selective inhibitor. 1,2,4-Trimethoxybenzene can markedly suppress Nigericin (HY-127019) or ATP (HY-B2176)-induced NLRP3 inflammasome activation, thus decreasing caspase-1 activation and IL-1β secretion. 1,2,4-Trimethoxybenzene specifically inhibits the activation of NLRP3 inflammasome without affecting absent in melanoma 2 (AIM2) inflammasome activation. 1,2,4-Trimethoxybenzene inhibits oligomerization of the apoptosis-associated speck-like protein containing a CARD (ASC) and protein-protein interaction between NLRP3 and ASC, thus blocking NLRP3 inflammasome assembly. 1,2,4-Trimethoxybenzene can be used for the study of experimental autoimmune encephalomyelitis (EAE), multiple sclerosis, and type 2 diabetes[1][2][3].

IC50 & Target[1]

NLRP3

 

Caspase-1

 

IL-1β

 

In Vitro

1,2,4-Trimethoxybenzene (0.5-1 mM, 1.5 h) significantly inhibits Nigericin (HY-127019) and Lipopolysaccharides (HY-D1056) (LPS)-induced NLRP3 inflammasome activation in immortalized murine bone marrow-derived macrophages (iBMDMs), manifested as reduced caspase-1 (Casp-1) cleavage and IL-1β secretion[1].
1,2,4-Trimethoxybenzene (1 mM, 75-90 min) inhibits LPS and ATP-induced NLRP3 activation in iBMDMs, primary microglia, and Primary macrophages cells[1].
1,2,4-Trimethoxybenzene (75-90 min) inhibits nigericin-induced NLRP3 activation in iBMDMs and primary macrophages, while 1,2,3-TTB had no inhibitory effect, indicating that the inhibitory activity is structure-dependent[1].
1,2,4-Trimethoxybenzene (45 min-2 h) does not inhibit LPS and poly(dA:dT)-induced activation of AIM2 inflammasome in primary peritoneal macrophages and iBMDMs[1].
1,2,4-Trimethoxybenzene (1 h) reduces the formation of ASC specks in iBMDMs and Primary microglia induced by LPS and nigericin: immunofluorescence showed a significant reduction in the number of ASC specks; DSS crosslinking experiments showed an increase in soluble ASCs and a decrease in insoluble ASCs[1].
1,2,4-Trimethoxybenzene (1 h) blocks the protein-protein interaction between NLRP3 and ASC in LPS-induced iBMDMs[1].
1,2,4-Trimethoxybenzene (1 h) inhibits LPS and nigericin-induced NLRP3 oligomerization of iBMDMs and primary macrophages: DSS crosslinking experiments showed reduced formation of NLRP3 monomers, dimers and higher oligomers[1].

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

1,2,4-Trimethoxybenzene Related Antibodies

Western Blot Analysis[1]

Cell Line: Immortalized murine bone marrow-derived macrophages (iBMDMs)
Concentration: 0.5 mM, 1 mM
Incubation Time: 1.5 h
Result: Caspase-1 (Casp-1) cleavage and IL-1β secretion are reduced.
In Vivo

1,2,4-Trimethoxybenzene (200 mg/kg, p.o., once daily for 17 days) significantly alleviates clinical symptoms, weight loss, and demyelinating pathology in EAE model mice[1].
1,2,4-Trimethoxybenzene (50-100 mg/kg, p.o., once daily for 3 days) enhances the extinction of fear memories and alleviates PTSD-related anxiety and depression-like behaviors in mice by inhibiting the NLRP3 inflammasome[2].
1,2,4-Trimethoxybenzene (50-200 mg/kg, p.o., once daily for 8 weeks) improves T2DM-related cognitive dysfunction by inhibiting NLRP3 inflammasome activation and regulating gut microbiota in type 2 diabetic rats[3].

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

Animal Model: Female C57BL/6 mice (6-8 weeks old) were subcutaneously injected with 150 μg of MOG35-55 peptide, and intraperitoneally injected with 200 ng of pertussis toxin on the day of immunization (day 0) and day 2, to simulate EAE[1].
Dosage: 200 mg/kg
Administration: P.o., once daily for 17 days
Result: The incidence of end-stage renal disease (ESRD) decreased, and clinical symptoms were significantly alleviated.
Significantly reduced weight loss indicates a reduction in systemic inflammatory response.
The area of myelin basic protein (MBP) positive in spinal cord sections was significantly larger than in the control group, indicating a reduced degree of demyelination.
The percentage of demyelinated area was significantly lower than in the control group, confirming the protection of myelin structure.
ASC specks were significantly reduced in spinal cord sections, suggesting that NLRP3 inflammasome activation was inhibited.
The expression of NLRP3, ASC, and cleaved caspase-1 proteins was downregulated in spinal cord tissue.
The mRNA expression of pro-inflammatory cytokines IFN-γ and IL-17a and the chemokine CCL-5 was decreased in the spinal cord, while the expression of the anti-inflammatory cytokine IL-4 was upregulated.
Animal Model: Male C57BL/6 mice (8 weeks old) were intraperitoneally injected with lipopolysaccharide (LPS, 2 mg/kg/d) for 3 consecutive days to induce depressive-like behavior[2].
Dosage: 50 mg/kg, 100 mg/kg
Administration: P.o., once daily for 3 days
Result: Sucrose preference was significantly increased (with improved depressive-like behavior), and immobility time in the tail suspension test (TST) and forced swimming test (FST) was significantly reduced.
Activation of the hippocampal NLRP3 inflammasome was inhibited (e.g., reduced expression of cleaved IL-1β, cleaved caspase-1, and ASC spot formation).
Animal Model: Male Sprague-Dawley rats (8 weeks old, 200 g) were first given a high-sugar, high-fat diet for 5 weeks, and then type 2 diabetes (T2DM) was induced by intraperitoneal injection of streptozotocin (STZ, 30 mg/kg)[3].
Dosage: 50 mg/kg, 100 mg/kg, 200 mg/kg
Administration: P.o., once daily for 8 weeks
Result: Significant improvements were observed in blood glucose levels (FBG, OGTT-AUC), insulin resistance index (HOMA-IR), and blood lipids (TC, TG, LDL-C) in rats, along with a decrease in oxidative stress markers (MDA).
Shortened escape latency and increased target quadrant time indicate enhanced learning and memory abilities.
Improved neuronal structure was observed in the hippocampal CA1 region, with ELISA detecting elevated BDNF levels and decreased AChE levels in the hippocampus.
Inhibition of the hippocampal NLRP3 inflammasome pathway (e.g., reduced expression of NLRP3, ASC, caspase-1, GSDMD, and IL-1β).
Molecular Weight

168.19

Formula

C9H12O3
CAS No.
Appearance

Liquid

SMILES

COC(C(OC)=C1)=CC=C1OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
Purity & Documentation
References
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1,2,4-Trimethoxybenzene Related Classifications

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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.

Keywords:

1,2,4-Trimethoxybenzene135-77-3NOD-like Receptor (NLR)CaspaseInterleukin RelatedILessential oilsNLRP3 inflammasomeASCexperimental autoimmune encephalomyelitisInhibitorinhibitorinhibit

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