Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 179 | 5日内发货 | ||
5 mg | ¥ 272 | 5日内发货 | ||
10 mg | ¥ 497 | 5日内发货 | ||
25 mg | ¥ 946 | 5日内发货 | ||
1 mL * 10 mM (in DMSO) | ¥ 298 | 5日内发货 |
SB 203580 hydrochloride 的其他形式现货产品:
产品描述 | Adezmapimod (SB 203580) hydrochloride is a selective ATP-competitive inhibitor of p38 MAPK, displaying IC50 values of 50 nM for SAPK2a/p38 and 500 nM for SAPK2b/p38β2. This compound also inhibits LCK, GSK3β, and PKBα, albeit with IC50 values 100-500 times higher than those for SAPK2a/p38. Additionally, Adezmapimod hydrochloride acts as an activator of autophagy and mitophagy [1]. |
体外活性 | 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. |
体内活性 | 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). |
分子量 | 413.9 |
分子式 | C21H17ClFN3OS |
CAS No. | 869185-85-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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