Adezmapimod,869185-85-3

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Adezmapimod hydrochloride

CAS No. : 869185-85-3

MCE 国际站：Adezmapimod hydrochloride

产品活性：Adezmapimod (SB 203580) hydrochloride 是一种选择性的，ATP 竞争性的 p38 MAPK 抑制剂，对 SAPK2a/p38 和 SAPK2b/p38β2 的 IC₅₀ 分别为 50 nM 和 500 nM。Adezmapimod hydrochloride 抑制 LCK，GSK3β 和 PKBα，IC₅₀ 比 SAPK2a/p38 高 100-500 倍。Adezmapimod hydrochloride 是一种自噬 (autophagy) 和有丝分裂 (mitophagy) 激活剂。

研究领域：MAPK/ERK Pathway | Autophagy

作用靶点：p38 MAPK | Autophagy | Mitophagy

In Vitro: Adezmapimod hydrochloride (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC₅₀ of 3-5 μM.
Adezmapimod hydrochloride blocks PKB phosphorylation (IC₅₀ 3-5 μM). Adezmapimod hydrochloride inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells.

In Vivo: Adezmapimod hydrochloride (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel.

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