产品说明书
BI-D1870
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同义名 : | - |
| CAS号 : | 501437-28-1 | |
| 货号 : | A153763 | |
| 分子式 : | C19H23F2N5O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 391.415 | |
| MDL号 : | MFCD11223662 | |
| 存储条件： |
粉末 Keep in dark place,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: 4 mg/mL(10.22 mM)，配合低频超声助溶，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： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | RSK (p90 ribosomal S6 kinase) is a member of the AGC subfamily that is activated by the mitogen-activated protein kinase in response to extracellular agonists. BI-D1870 is a specific inhibitor of RSK isoforms with >500-fold greater selectivity over other AGC kinases. In the kinase assays with 100 μM ATP, BI-D1870 inhibited RSK1 and RSK2 with IC50 values of 10 nM and 20 nM, respectively. When the concentration of ATP decreased to 10 μM, the IC50 values of BI-D1870 was reduced to 5 nM for RSK1 and 10 nM for RSK2. BI-D1870 also inhibited an active mutant of RSK2 lacking the C-terminal kinase catalytic domain with an IC50 of 30 nM. In HEK-293 cells that were incubated with 10 μM BI-D1870 for 15 min prior to the stimulation with 20 ng/ml PMA, the PMA-induced phosphorylation of GSK3α and GSK3β was strongly inhibited compared to non- BI-D1870-treated cells. When HEK-293 cells were pretreated with 10 μM BI-D1870 for 30 min before PMA stimulation, the phosphorylation of LKB1 was inhibited with an IC50 value of approximately 1 μM. In serum-deprived Rat-2 cells that were incubated with BI-D1870 for 30 min, EGF-induced phosphorylation of LKB1 at Ser431 was inhibited with an IC50 of around 1 μM. Incubation of Rat-2 cells with 10 μM BI-D1870 for 30 min led to 50% less phosphorylation of ERK1 and ERK2 compared to the level that was observed immediately followed the EGF stimulation. In experimental autoimmune encephalomyelitis mice, i.p. administration of BI-D1870 (0.5 mg/kg) every other day for 11 days resulted in delayed neural deficit, decreased number of CD4+ T cells that infiltrated into the CNS, and reduced mRNA levels of Ccr6 in Th17 cells. | ||
| 作用机制 | BI-D1870 is a RSK inhibitor derived from dihydropteridinones. BI-D1870 competes with ATP to inhibit the N-terminal AGC kinase domain. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| 22RV1 | Growth Inhibition Assay | IC50=8.61786 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=14.8353 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=4.61444 μM | SANGER | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.55mL 0.51mL 0.26mL |
12.77mL 2.55mL 1.28mL |
25.55mL 5.11mL 2.55mL |
