TRAF-STOP inhibitor 6877002
CAS No. : 433249-94-6
| Size | Price | Stock |
|---|---|---|
| 5mg | $55 | In-stock |
| 10mg | $76 | In-stock |
| 25mg | $165 | In-stock |
| 50mg | $297 | In-stock |
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| Cat. No. : | HY-110247 |
| M.Wt: | 251.32 |
| Formula: | C17H17NO |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
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].
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].
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