C25-140 |
| カタログ番号GC34513 |
C25-140 は、クラス初の経口活性型でかなり選択的な TRAF6-Ubc13 阻害剤であり、TRAF6 に直接結合し、TRAF6 と Ubc13 との相互作用をブロックします。
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.
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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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