MLN2238

20S蛋白酶体抑制剂（β5亚基无细胞测定中的IC50=3.4nM）和MLN9708的活性代谢物；对β5亚基的选择性优于β1和β2亚基（IC50s分别为31和3,500nM）；结合酪蛋白水解蛋白酶P（Kd=5,700nM）；防止MRSA诱导的绵羊红细胞溶血（EC50=3,600nM）；抑制A375、H460、HCT116和HT-29细胞的增殖（IC50s分别为20、58、19和52nM）；抑制多发性骨髓瘤患者分离的PBMCs中的破骨细胞生成（IC50=4.8nM）；14毫克/千克剂量可降低CWR22前列腺癌小鼠异种移植模型中的肿瘤生长。A 20S proteasome inhibitor (IC50 = 3.4 nM in a cell-free assay for the β5 subunit) and an active metabolite of MLN9708; selective for the β5 subunit over the β1 and β2 subunits (IC50s = 31 and 3,500 nM, respectively); binds caseinolytic protease P (Kd = 5,700 nM); prevents MRSA-induced hemolysis of isolated ovine erythrocytes (EC50 = 3,600 nM); inhibits the proliferation of A375, H460, HCT116, and HT-29 cells (IC50s = 20, 58, 19, and 52 nM, respectively); inhibits osteoclastogenesis in PBMCs isolated from patients with multiple myeloma (IC50 = 4.8 nM); reduces tumor growth in a CWR22 prostate cancer mouse xenograft model at 14 mg/kg.