| Description | KRN2 bromide is a potent, selective inhibitor of nuclear factor of activated T cells (NFAT5, IC50= 0.1 μM). |
| In vitro | KRN2 bromide 以剂量依赖的方式抑制NF-κB p65与Nfat5启动子1的结合，并直接阻断NF-κB p65与Nfat5外显子1上游位点（碱基对-3000至+1）DNA结合序列的互作。KRN2 bromide 选择性抑制包括Nos2和Il6在内的促炎症基因表达，而不影响高盐诱导的NFAT5及其靶基因的表达[1]。 |
| In vivo | 在DBA/1J小鼠中，通过注射牛型II胶原蛋白进行免疫后，KRN2溴化物（3 mg/kg，腹腔注射）有效抑制了CIA及以先天免疫细胞为主的AIA，同时减少了促炎症细胞因子和自身抗体的产生，并降低了巨噬细胞的浸润[1]。 |
| Target activity | NFAT5:100 nM |
| molecular weight | 524.38 |
| Molecular formula | C27H23BrFNO4 |
| CAS | 1390654-28-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 8 mg/mL (15.26 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) |
| References | 1. Han EJ, et al. Suppression of NFAT5-mediated Inflammation and Chronic Arthritis by Novel κB-binding Inhibitors. EBioMedicine. 2017 Apr;18:261-273. |