2. Apoptosis NF-κB
  3. TNF Receptor NF-κB
  4. TRAF-STOP inhibitor 6877002

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.

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TRAF-STOP inhibitor 6877002 Chemical Structure

TRAF-STOP inhibitor 6877002 Chemical Structure

CAS No. : 433249-94-6

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Based on 1 publication(s) in Google Scholar

TRAF-STOP inhibitor 6877002 Related Antibodies

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1 Publications Citing Use of MCE TRAF-STOP inhibitor 6877002

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TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Description

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[1].

IC50 & Target

CD40-TRAF6 interaction; NF-κB
In Vitro

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.

TRAF-STOP inhibitor 6877002 Related Antibodies

Western Blot Analysis[1]

Cell Line: BMDMs
Concentration: 10 μM
Incubation Time: 10 min, 24 hours
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.
In Vivo

TRAF-STOP inhibitor 6877002 (10 μmol/kg; intraperitoneal injection; once a day; 6 weeks) retards the development of early atherosclerosis and reduces atherosclerotic plaque area in apolipoprotein E-deficient (Apoe-/-) mice[1].
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.

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].
Dosage: 10 μmol/kg (vehicle: PBS, 0.05% Tween 80, 5% dimethylsulfoxide)
Administration: Intraperitoneal injection, once a day, for 6 weeks
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.
Animal Model: Male apolipoprotein E-deficient (Apoe-/-) mice (12 weeks old), fed a normal chow diet to establish an atherosclerosis-prone model[1].
Dosage: 10 μmol/kg (vehicle: PBS, 0.05% Tween 80, 5% dimethylsulfoxide)
Administration: Intraperitoneal injection, once a day, for 6 weeks
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.
Animal Model: Male apolipoprotein E-deficient (Apoe-/-) mice (12 weeks old) with atherosclerosis model[1].
Dosage: 10 μmol/kg (packaged in recombinant high-density lipoprotein nanoparticles)
Administration: Administered via recombinant high-density lipoprotein nanoparticles, twice a week, for 6 weeks
Result: Reduced plaque volume in the aortic root and the number of macrophages in plaques.
Molecular Weight

251.32

Formula

C17H17NO
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=CC=C1)/C=C/NC2=C(C=CC(C)=C2)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9790 mL 19.8950 mL 39.7899 mL
5 mM 0.7958 mL 3.9790 mL 7.9580 mL
View the 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.

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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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (8.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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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    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:

TRAF-STOP inhibitor 6877002433249-94-6TNF ReceptorNF-κBTumor Necrosis Factor ReceptorTNFRNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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