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C25-140
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
C25-140图片
CAS NO:1358099-18-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
C25-140是一种一流的TRAF6-Ubc13相互作用的抑制剂,直接与TRAF6结合,阻断TRAF6和Ubc13的相互作用,从而降低TRAF6活性并对抗自身免疫。
Cas No.1358099-18-9
Canonical SMILESO=C(N1CCC(CC2=CC=CC=C2)CC1)CCC3=C(C)N(C4=NN5C(C=C4)=NN=C5C)N=C3C
分子式C26H31N7O
分子量457.57
溶解度DMSO : ≥ 130 mg/mL (284.11 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.