产品说明书
SB 203580
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同义名 : | RWJ 64809;Adezmapimod;SB203850;PB 203580 |
| CAS号 : | 152121-47-6 | |
| 货号 : | A248150 | |
| 分子式 : | C21H16FN3OS | |
| 纯度 : | 99%+ | |
| 分子量 : | 377.435 | |
| MDL号 : | MFCD00922198 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 18 mg/mL(47.69 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 4 mg/mL clear PO 0.5% CMC-Na 60 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | The stress-activated protein kinase (SAPK) p38 isoforms are mitogen-activated protein kinase (MAPK) family members. MAPKs act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development. SB 203580 is a p38 MAPK inhibitor. SB 203580 inhibited the ATPase activity of non-phosphorylated p38 MAPK with a Km of 9.6 mM. SB 203580 was competitive with ATP with a Ki of 21 nM, detected in a kinetic study of yeast expressed active p38 MAPK[3]. 24h treatment of SB 203580 dose-dependently inhibited IL-1β-induced PGE2 release with an EC50 of 0.18 μM[4]. SB 203580 was dissolved in drinking water at the concentration of 250 μM and orally administrated 0.4 ml/day to MRL/lpr mice aged from 14 to 22 weeks. SB203580 improved renal function by decreasing the levels of proteinuria and serum BUN, ameliorating the pathologic changes of kidney and reducing Ig and C3 depositions in the kidney. Moreover, hepatocytes necrosis, recruitment and proliferation of leucocytes in liver and spleen were found to be inhibited by administration of SB203580[5]. |
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| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| HCA2 | 2.5 μM | Function Assay | Inhibits p38 mediated MK2 activation | 17964780 | |
| Hela | Function Assay | Inhibits Tat-induced HIV1 LTR transactivation in human HeLa cells with IC50 of 0.1 μM | 18926711 | ||
| hESCs | 5 μM | Growth Inhibition Assay | Induces cardiomyogenic activity assessed as cell growth | 23602399 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.65mL 0.53mL 0.26mL |
13.25mL 2.65mL 1.32mL |
26.49mL 5.30mL 2.65mL |
