| Bioactivity | PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research[1][2]. |
| Invitro | PPI-2458 可有效抑制 HUVEC 增殖，GI50 为0.2 nM，在1 nM 时最大抑制率大于 95%[1]。PPI-2458 (0-100 nM, 6天)抑制 SU-DHL-16 细胞的增殖和MetAP-2[2]。 Cell Proliferation Assay[2] Cell Line: |
| In Vivo | PPI-2458 (0-50 mg/kg，口服，隔日一次)逆转 PG-PS (25 mg/kg, i.p) 诱导的关节炎模型中的关节肿胀和炎症[1]。PPI-2458 (0-3 mg/kg，鼻胃插管，隔日一次)可导致实验初代食蟹猴生发中心生发中心淋巴细胞减少[2]。PPI-2458 (0-100 mg/kg，口服，隔日一次)以剂量依赖的方式显著抑制肿瘤生长在SR肿瘤异种移植的严重联合免疫缺陷小鼠中[2]。 Animal Model: |
| Name | PPI-2458 |
| CAS | 431077-35-9 |
| Formula | C22H36N2O6 |
| Molar Mass | 424.53 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Bernier SG, et al. A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis. Proc Natl Acad Sci U S A. 2004 Jul 20;101(29):10768-73. [2]. Cooper AC, et al. A novel methionine aminopeptidase-2 inhibitor, PPI-2458, inhibits non-Hodgkin's lymphoma cell proliferation in vitro and in vivo. Clin Cancer Res. 2006 Apr 15;12(8):2583-90. |