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KRN2 (bromide) is a selective inhibitor of nuclear factor of activated T cells (NFAT5) , with an IC 50 of 0.1 μM.
In Vitro
KRN2 selectively suppresses the expression of pro-inflammatory genes, including Nos2 and Il6, without hampering high-salt-induced NFAT5 and its target gene expressions. KRN2 dose-dependently inhibits the NF-κB p65 binding to Nfat5 promoter 1 and directly blocks the interaction between NF-κB p65 and its DNA binding sequence in the upstream site (base pairs -3000 to +1) of Nfat5 exon 1. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
KRN2 (3 mg/kg, i.p., daily for 2 weeks) effectively suppresses AIA in which innate immune cells play a predominant role . KRN2 (3 mg/kg, i.p., daily) effectively suppresses CIA as well as AIA in mice, decreasing the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 8-week-old C57BL/6 mice injected intradermally with 2 mg of complete Freund's adjuvant . 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 . Dosage: 3 mg/kg. Administration: Peritoneally (i.p.) daily. Result: Effective in suppressing CIA as well as AIA in mice, decreasing the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration.
Form:Solid
IC50& Target:IC50: 100 nM (NFAT5)