SB 203580CAS号: 152121-47-6分子式: C21H16FN3OS分子量: 377.44描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
SB203580是一种p38 MAPK抑制剂,在THP-1细胞中IC50为0.3-0.5μM,对SAPK3(106T)和SAPK4(106T)选择性低10倍,且阻断PKB磷酸化,IC50为3-5μM。SB203580是第一个被报道的p38抑制剂。 |
| 纯度 |
>98%
|
| 储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 别名 |
Adezmapimod;RWJ 64809
|
| 外观 |
white to off-white powder
|
| 可溶性/溶解性 |
DMSO:43 mg/mL (113.92 mM)
|
| 生物活性 | |
| 靶点 |
p38 MAPK;PKB
|
| In vitro(体外研究) |
SB203580 inhibits 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. SB203580 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range. SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity. SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells.
|
| In vivo(体内研究) |
SB203580 protects pig myocardium against ischemic injury in an in vivo model. SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE).
|
分子结构图
