AdezmaPimod (SB 203580) hydrochloride 是一种选择性的，ATP 竞争性的p38 MAPK抑制剂，其对于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 也是一种自噬 (Autophagy) 和有丝分裂 (Mitophagy) 激活剂。

Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC 50 s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC 50 s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is also an activator of autophagy and mitophagy [1].

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 proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells induced by IL-2, with an IC 50 of 3-5 μM [1]. Adezmapimod hydrochloride blocks PKB phosphorylation (IC 50 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 [1]. Cell Proliferation Assay [1] Cell Line: CT6, BA/F3 cell line F7, and PBMC/T cells Concentration: 0-30 μM Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2 Result: Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC 50 of 3-5 μM. Western Blot Analysis [1] Cell Line: CT6 cells, activated human T cells, and BA/F3 F7 cells Concentration: 0-30 μM Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min Result: Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.

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 treated in parallel [1]. Animal Model: Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors [1] Dosage: 5 mg/kg/day Administration: Intra peritoneal injected daily for 16 consecutive days Result: After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).

869185-85-3

C21H17ClFN3OS

413.9

SB 203580 hydrochloride

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years