KRN2-bromide - NFAT5 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKRN2 bromideCat. No.: HY-112125ACAS No.: 1390654-28-0分式: CHBrFNO分量: 524.38作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 60 mg/mL (114.42 mM)* means soluble, but satu

2、ration unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9070 mL 9.5351 mL 19.0701 mL5 mM 0.3814 mL 1.9070 mL 3.8140 mL10 mM 0.1907 mL 0.9535 mL 1.9070 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 KRN2 (bromide)选择性的 T 细胞激活核因 (NFAT5) 的抑制剂，其IC50 值为100 nM。 KRN2具有治疗NFA

3、T5-介导的慢性关节炎的潜能。IC50 & Target IC50: 100 nM (NFAT5) 1体外研究KRN2 selectively suppresses the expression of pro-inflammatory genes, including Nos2 and Il6, without1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEhampering high-salt-induced NFAT5 and its target gene expressions 1.KRN2 dose-dependently inhib

4、its the NF-B p65 binding to Nfat5 promoter 1 and directly blocks theinteraction between NF-B p65 and its DNA binding sequence in the upstream site (base pairs -3000 to +1)of Nfat5 exon 1 1.体内研究 KRN2 (3 mg/kg, i.p., daily for 2 weeks) effectively suppresses AIA in which innate immune cells play apred

5、ominant role 1.KRN2 (3 mg/kg, i.p., daily) effectively suppresses CIA as well as AIA in mice, decreasing the production ofpro-inflammatory cytokines and autoantibodies as well as macrophage infiltration 1.Animal Model: 8-week-old C57BL/6 mice injected intradermally with 2 mg of complete Freunds adju

6、vant1.Dosage: 3 mg/kg.Administration: Peritoneally (i.p.) daily for 2 weeks.Result: Effective in suppressing AIA.Animal Model: 8-week-old DBA/1Jmice immunized with bovine type II collagen 1.Dosage: 3 mg/kg.Administration: Peritoneally (i.p.) daily.Result: Effective in suppressing CIA as well as AIA

7、in mice, decreasing the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration.REFERENCES1. Han EJ, et al. Suppression of NFAT5-mediated Inflammation and Chronic Arthritis by Novel B-binding Inhibitors. EBioMedicine. 2017Apr;18:261-273.McePdfHeightCaution: Product has not been fully validated for medical applications.For research us