C25-140 - TRAF6-Ubc13 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEC25-140Cat. No.: HY-120934CAS No.: 1358099-18-9分式: CHNO分量: 457.57作靶點: TNF Receptor; E1/E2/E3 Enzyme作通路: Apoptosis; Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 1

2、30 mg/mL (284.11 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.1855 mL 10.9273 mL 21.8546 mL5 mM 0.4371 mL 2.1855 mL 4.3709 mL10 mM 0.2185 mL 1.0927 mL 2.1855 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添?/p>

3、助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.17 mg/mL (4.74 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.17 mg/mL (4.74 mM); Clear solution3. 請依序添加每種溶劑： 10%

4、 DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.17 mg/mL (4.74 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 C25-140種流的 TRAF6Ubc13 相互作的抑制劑，直接與 TRAF6 結(jié)合，阻斷 TRAF6 和 Ubc13 的相互作，從降低 TRAF6 活性并對抗免疫 1。IC50 & Target TRAF6-Ubc13 1體外研究 C25-140 dose-dependently impedes TRAF6-Ubc13

5、interaction 1.C25-140 (10-30 M; 2 hours) effectively reduces TRAF6-mediated ubiquitin chain formation 1.C25-140 affects TNF-induced phosphorylation of IB as well as NF-B-induced target gene expression 1.C25-140 efficiently inhibits IL-1- and TNF-mediated receptor signaling in the context of cytokine

6、 activation1.Western Blot Analysis 1Cell Line: TRAF6WTConcentration: 10 M, 20 M, 30 MIncubation Time: 2 hoursResult: Effectively reduced TRAF6-mediated ubiquitin chain formation.體內(nèi)研究C25-140 (1.5 mg/kg; topically to the shaved back and the right ear; twice daily for 6 days) amelioratessymptoms of aut

7、oimmune psoriasis in R 837-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 RAdisease outcome in Collagen-induced arthritis (CIA) model 1.Animal Model: R 837-induced psoriasis mouse model (male BALB/c mice) 1Dosage: 1.5 m

8、g/kgAdministration: Topically to the shaved back and the right ear; twice daily for 6 daysResult: Showed a dose-dependent improvement of RA disease outcome.Animal Model: Collagen-induced arthritis (CIA) model in DBA1/J mice 1Dosage: 6 mg/kg, 10 mg/kg, 14 mg/kgAdministration: Given i.p.; twice daily

9、for 14 daysResult: Ameliorated the arthritic index to almost baseline levels in this efficacy model at doses of2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE10 and 14 mg/kg. Dose-dependently improved symptoms of RA including inflammationand structural damage.REFERENCES1. Brenke JK, et al. Targeting TRAF6 E3 ligase activity with a small-molecule inhibitor combats autoimmunity. J Biol Chem. 2018 Aug24;293(34):13191-13203.McePdfHeightCaution: Product has not been fully validated for