ONX 0914

免疫蛋白酶体β5i(LMP7)亚基的选择性抑制剂（小鼠和人类的IC50s分别为65和73nM），对组成型蛋白酶体β5亚基的活性明显较弱（小鼠和人类的IC50s分别为0.92和1.04µM）；阻止促炎细胞因子的产生并抑制TH1和TH17细胞分化；减轻多种自身免疫性疾病实验模型以及一些血液系统恶性肿瘤的病情进展。A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC50s = 65 and 73 nM for mouse and human, respectively) that demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC50s = 0.92 and 1.04 µM for mouse and human, respectively); blocks the production of proinflammatory cytokines and inhibits TH1 and TH17 cell differentiation; attenuates disease progression in several experimental models of autoimmune disorders as well as in some hematologic malignancies.