KN-93

KN-93, un inibitore di CaMK2, riduce la differenziazione delle cellule B e la produzione di IgG da parte delle plasmacellule differenziate, e inibisce l'espressione di Blimp-1 nelle cellule B.[2]

KN93 mostra un effetto protettivo sulla pancreatite acuta (PA) in modo dose-dipendente, senza effetti collaterali tossici sui topi.[3]

• Linee cellulari

  human B cells isolated from lupus nephritis (LN) patients

• Concentrazioni

  5 μM

• Tempo di incubazione

  --

• Metodo

  For B-cell differentiation, isolated naive B cells were cultured in Roswell Park Memorial Institute (RPMI) 1640 supplemented with 10% fetal bovine serum (FBS) and 1% penicillin/streptomycin. Cells were stimulated with antihuman IgM (5 μg/ml) and antihuman CD40 (1 μg/ml) antibodies in the presence of interleukin (IL)-2 (20 ng/ml), IL-4 (25 ng/ml) and IL-21 (50 ng/ml) for 8 days. For signaling study, cells treated with KN-93 (1 μM) to study the roles of CaMK2 in human B-cell differentiation. Proteins were loaded to sodium dodecyl sulfate (SDS)-polyacrylamide gels and electrotransferred onto polyvinylidine difluoride membranes after separation. Membranes were blocked with 5% bovine serum albumin in TBST buffer and incubated with primary antibodies against ORAI1, ORAI2, STIM2, Blimp-1, and p-CaMK2, at 4°C overnight. Membranes were incubated with anti-GAPDH primary antibody and used as internal control. Membranes were then washed with TBST and incubated with horseradish-peroxidase-conjugated antirabbit or antimouse IgG at room temperature for 60 min. Signals were detected by enhanced chemiluminescence analysis kit.

• Modelli animali

  mice of acute pancreatitis (AP) model

• Dosaggi

  5, 10, 20 mg/kg

• Somministrazione

  i.p.