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Ralimetinib dimesylate

CAS No. : 862507-23-1

MCE 站：Ralimetinib dimesylate

产品活性：Ralimetinib dimesylate (LY2228820 dimesylate) 是一种选择性，ATP竞争性的 p38 MAPK α/β 抑制剂，IC₅₀ 分别为5.3 和 3.2 nM。

研究领域：MAPK/ERK Pathway  |  Autophagy  |  Apoptosis

作用靶点：p38 MAPK  |  Autophagy  |  Apoptosis

In Vitro: Ralimetinib dimesylate inhibits p38α, as well as the level of phosphoMAPKAPK-2 (pMK2) in RAW 264.7 cells, with IC₅₀ values of 7 nM ａnd 34.3 nM, respectively. Furthermore, Ralimetinib dimesylate inhibits lipopolysaccharide (LPS)-induced TNFα formation in murine peritoneal macrophages, with IC₅₀ of 5.2 nM. In multiple myeloma (MM) cells, including INA6, RPMI-8226, U266, ａnd RPMI-Dox40, Ralimetinib dimesylate (LY2228820) (200 nM-800 nM) significantly blocks p38MAPK signaling, as revealed by its inhibition on phosphorylation of HSP27, a downstream target of p38MAPK, without affecting the expression level of HSP27. Ralimetinib dimesylate (200 nM-400 nM) enhances bortezomib-induced cytotoxicity ａnd apoptosis, but Ralimetinib dimesylate alone doesn＇t inhibit the growth of MM.1S cells. Ralimetinib dimesylate (200 nM-800 nM) also inhibits secretion of IL-6 ａnd MIP-1α in long-term BM stromal cells (LT-BMSCs), BM mononuclear cells (BMMNCs), peripheral blood (PB) CD138⁺, CD138^- or PB CD14⁺ cells. Ralimetinib dimesylate (400 nM-800 nM) also blocks osteoclastogenesis from CD14⁺ cells.

In Vivo: In LPS-induced mice, Ralimetinib dimesylate effectively inhibits the formation of TNFα with a threshold minimum 50% effective dose (TMED₅₀) less than 1 mg/kg. In a rat model of collagen-inducedarthritis (CIA), Ralimetinib dimesylate displays potent effects on paw swelling, bone erosion, ａnd cartilage destruction, with a threshold minimum 50% effective dose (TMED₅₀)of 1.5 mg/kg. Ralimetinib dimesylate inhibits tumor phospho-MK2 in a dose-dependent manner (TED₅₀=1.95 mg/kg, TED₇₀=11.17 mg/kg) in mice implanted with B16-F10 melanoma. Ralimetinib dimesylate inhibits MK2 phosphorylation: mouse in vivo TED₅₀=1.01 mg/kg (compound exposure approximately 100 nM) ａnd human ex vivo IC₅₀=0.12 μM with either mouse or human PBMC.

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