TRAF-STOP inhibitor 6877002
Based on 4 publication(s) in Google Scholar
TRAF-STOP inhibitor 6877002 is a selective CD40-TRAF6 interaction inhibitor. TRAF-STOP inhibitor 6877002 exerts anti-atherosclerotic activity by blocking the CD40-TRAF6 signaling pathway, inhibiting classical monocyte activation, leukocyte recruitment, and macrophage activation and migration. TRAF-STOP inhibitor 6877002 reduces the phosphorylation levels of signaling intermediates in the canonical NF-κB pathway.
For research use only. We do not sell to patients.
- Purity: 99.67%
- CAS No.: 433249-94-6
- Formula: C17H17NO
- Molecular Weight:251.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) TRAF-STOP inhibitor 6877002
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Biological Activity
CD40-TRAF6 interaction; NF-κB
TRAF-STOP inhibitor 6877002 (10 μM; 10 min-24 h) reduces the CD40-induced expression of TNF-α, IL-1β, IL-6, IL-10, IL-12, and inducible nitric oxide synthase (iNOS) in bone marrow-derived macrophages (BMDMs). TRAF-STOP inhibitor 6877002 reduces the CD40-induced phosphorylation of Tak1 and NF-κB p65. TRAF-STOP inhibitor 6877002 also reduces the expression of the chemokine-chemokine receptor pairs CCL2-CCR2 and CCL5-CCR5 in bone marrow-derived macrophages (BMDMs)[1].
TRAF-STOP inhibitor 6877002 (10 μM) reduces CD36 expression in bone marrow-derived macrophages (BMDMs), resulting in decreased uptake of oxidized low-density lipoprotein and reduced macrophage foam cell formation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BMDMs
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Concentration:10 μM
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Incubation Time:10 min, 24 hours
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Result:Reduced the CD40-induced phosphorylation of Tak1 and NF-κB p65, whereas the levels of NF-κB2 p52 and the phosphorylation of ERK1/2 were not affected.
TRAF-STOP inhibitor 6877002 (10 μmol/kg; intraperitoneal injection; once a day; 6 weeks) halts the progression of established atherosclerosis, induces a stable plaque phenotype, reduces macrophage number and proliferation, decreases the size of necrotic cores, reduces the number of neutrophils and T cells, and increases collagen and αSMA+ smooth muscle cell content in atherosclerotic plaques in apolipoprotein E-deficient (Apoe-/-) mice[1].
TRAF-STOP inhibitor 6877002 (10 μmol/kg; administered via recombinant high-density lipoprotein nanoparticles; twice a week; 6 weeks) reduces plaque volume in the aortic root and the number of macrophages in plaques in apolipoprotein E-deficient (Apoe-/-) mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male apolipoprotein E-deficient (Apoe-/-) mice (22 weeks old), with advanced atherosclerotic lesions already present in the aortic arch to establish an established atherosclerosis model[1].
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Dosage:10 μmol/kg (vehicle: PBS, 0.05% Tween 80, 5% dimethylsulfoxide)
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Administration:Intraperitoneal injection, once a day, for 6 weeks
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Result:Halted the progression of established atherosclerosis, reduced the total atherosclerotic plaque area in the aortic arch and aortic root. The atherosclerotic plaques exhibited a stable phenotype with decreased macrophage number and proliferation, smaller necrotic cores, fewer neutrophils and T cells, and increased collagen and αSMA+ smooth muscle cell content.
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Animal Model:Male apolipoprotein E-deficient (Apoe-/-) mice (12 weeks old), fed a normal chow diet to establish an atherosclerosis-prone model[1].
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Dosage:10 μmol/kg (vehicle: PBS, 0.05% Tween 80, 5% dimethylsulfoxide)
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Administration:Intraperitoneal injection, once a day, for 6 weeks
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Result:Retarded the development of early atherosclerosis, reduced atherosclerotic plaque area in the aortic arch, and the plaques contained fewer macrophages, T cells, and neutrophils. There were no changes in the number of proliferating or apoptotic cells, plaque smooth muscle cell or collagen content.
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Animal Model:Male apolipoprotein E-deficient (Apoe-/-) mice (12 weeks old) with atherosclerosis model[1].
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Dosage:10 μmol/kg (packaged in recombinant high-density lipoprotein nanoparticles)
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Administration:Administered via recombinant high-density lipoprotein nanoparticles, twice a week, for 6 weeks
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Result:Reduced plaque volume in the aortic root and the number of macrophages in plaques.
Chemical Information
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CAS No. 433249-94-6
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Appearance Solid
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Molecular Weight 251.32
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Formula C17H17NO
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=CC=C1)/C=C/NC2=C(C=CC(C)=C2)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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J Control Release
Fibrin gel-based co-delivery of self-adjuvant tumor vaccine and PD-1 blockade for post-surgical gastric cancer immunotherapy. [Abstract]2026 Mar 10:391:114629. PMID: 41544668 -
Cell Rep
2024 Aug 22;43(9):114664. PMID: 39178113 -
Front Immunol
Fusobacterium nucleatum drives CD40-mediated dendritic cell activation and Th17/Treg imbalance to exacerbate intestinal inflammation in Crohn's disease. [Abstract]2026 Jan 6:16:1712971. PMID: 41567217 -
Sci Rep
Mitigating cardiac allograft vasculopathy in a murine model via CD40-TRAF6 blockade and cyclosporin A synergy. [Abstract]2025 Jul 1;15(1):22327. PMID: 40595221
Solvent & Solubility
DMSO : 100 mg/mL (397.90 mM; Need ultrasonic; 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, 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (8.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (398 KB)
- English - EN (398 KB)
- Français - FR (398 KB)
- Deutsch - DE (398 KB)
- Norwegian - NO (398 KB)
- Español - ES (398 KB)
- Swedish - SV (398 KB)
- Italian - IT (398 KB)
- Korean - KR (398 KB)
- Portuguese - PT (398 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, 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 | 3.9790 mL | 19.8950 mL | 39.7899 mL | 99.4748 mL |
| 5 mM | 0.7958 mL | 3.9790 mL | 7.9580 mL | 19.8950 mL | |
| 10 mM | 0.3979 mL | 1.9895 mL | 3.9790 mL | 9.9475 mL | |
| 15 mM | 0.2653 mL | 1.3263 mL | 2.6527 mL | 6.6317 mL | |
| 20 mM | 0.1989 mL | 0.9947 mL | 1.9895 mL | 4.9737 mL | |
| 25 mM | 0.1592 mL | 0.7958 mL | 1.5916 mL | 3.9790 mL | |
| 30 mM | 0.1326 mL | 0.6632 mL | 1.3263 mL | 3.3158 mL | |
| 40 mM | 0.0995 mL | 0.4974 mL | 0.9947 mL | 2.4869 mL | |
| 50 mM | 0.0796 mL | 0.3979 mL | 0.7958 mL | 1.9895 mL | |
| 60 mM | 0.0663 mL | 0.3316 mL | 0.6632 mL | 1.6579 mL | |
| 80 mM | 0.0497 mL | 0.2487 mL | 0.4974 mL | 1.2434 mL | |
| 100 mM | 0.0398 mL | 0.1989 mL | 0.3979 mL | 0.9947 mL |
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