C25-140 |
Catalog No.GC34513 |
C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1358099-18-9
Sample solution is provided at 25 µL, 10mM.
C25-140, a first-in-class TRAF6-Ubc13 inhibitor, directly binds to TRAF6, thereby blocks the interaction of TRAF6 with Ubc13 and as a consequence lowers TRAF6 activity and combats autoimmunity[1]. TRAF6-Ubc13[1]
C25-140 dose-dependently impedes TRAF6-Ubc13 interaction[1].C25-140 (10-30 μM; 2 hours) effectively reduces TRAF6-mediated ubiquitin chain formation[1].C25-140 affects TNFα-induced phosphorylation of IκBα as well as NF-κB-induced target gene expression[1].C25-140 efficiently inhibits IL-1β- and TNFα-mediated receptor signaling in the context of cytokine activation[1]. Western Blot Analysis[1] Cell Line: TRAF6WT
C25-140 (~1.5 mg/kg; topically to the shaved back and the right ear; twice daily for 6 days) ameliorates symptoms of autoimmune psoriasis in Imiquimod-induced psoriasis mouse model[1].C25-140 (6-14 mg/kg; given i.p.; twice daily for 14 days) shows a dose-dependent improvement of RA disease outcome in Collagen-induced arthritis (CIA) model[1]. Animal Model: Imiquimod-induced psoriasis mouse model (male BALB/c mice)[1]
[1]. Brenke JK, et al. Targeting TRAF6 E3 ligase activity with a small-molecule inhibitor combats autoimmunity. J Biol Chem. 2018 Aug 24;293(34):13191-13203.
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