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BI-D1870

现货
Catalog No.
B2227
P90 RSK抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,600.00
现货
5mg
¥ 1,200.00
现货
10mg
¥ 1,900.00
现货
50mg
¥ 4,700.00
现货

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Background

BI-D1870 is a cell-permeable inhibitor of the p90 RSK isoforms with IC50 values of 31nM, 24nM, 18nM and 15nM for RSK1, RSK2, RSK3 and RSK4 respectively [1].

BI-D1870 is a derivative of dihydropteridinone and found to be a remarkably specific inhibitor of RSK isoforms. It is an ATP-competitive inhibitor. When the concentrations of ATP are 10μM and 100μM, the IC50 values of BI-D1870 against RSK1 and RSK2 are 5nM, 10nM and 10nM, 20nM, respectively. BI-D1870 also inhibits RSK3 and RSK4 with IC50 values of 18nM and 15nM respectively, when ATP is 100μM. The inhibition activity of BI-D1870 against RSK is more than 500-fold greater than some other AGC kinases suggesting BI-D1870 as a specific inhibitor of RSK. In addition, BI-D1870 is reported to induce the phosphorylation of ERK1/ERK2 and the subsequent phosphorylation of CREB in Rat-2 cells [1].

References:
[1] Sapkota G, Cummings L, Newell F, et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem. J, 2007, 401: 29-38.

文献引用

1. Sechi M, Lall RK, et al. "Fisetin targets YB-1/RSK axis independent of its effect on ERK signaling:insights from in vitro and in vivo melanoma models." Sci Rep. 2018 Oct 24;8(1):15726. PMID:30356079

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt391.42
Cas No.501437-28-1
FormulaC19H23F2N5O2
Solubility≥19.55mg/mL in DMSO
Chemical Name2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one
SDFDownload SDF
Canonical SMILESCC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

HEK-293细胞

溶解方法

在DMSO中的溶解度>19.6mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0-10 μM; 15, 30, 60, 120和240 min

应用

在HEK-293细胞中,BI-D1870大大抑制了PMA诱导的GSK3α和GSK3β的磷酸化。BI-D1870还抑制PMA诱导的GSK3亚型和另一种RSK底物,蛋白激酶LKB1的磷酸化,IC50约为1μM。

动物实验[2]:

动物模型

实验性自身免疫性脑脊髓炎(EAE)小鼠

剂量

0.5 mg/kg; 腹腔注射; 隔天给药,持续11天

应用

在用MOG肽免疫的EAE小鼠中,BI-D1870通过减少TH1和TH17细胞渗入CNS并降低TH17细胞中Ccr6的mRNA水平来保护小鼠免于EAE。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1] Sapkota G, Cummings L, Newell F, et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem. J, 2007, 401: 29-38.

[2]. Takada I1, Yogiashi Y2, Makishima M3. et al. The ribosomal S6 kinase inhibitor BI-D1870 ameliorated experimental autoimmune encephalomyelitis in mice. Immunobiology. 2016 Feb;221(2):188-92.

生物活性

Description BI-D1870是一种S6核糖体的ATP竞争性抑制剂,对RSK1/2/3/4的IC50 值分别为31 nM/24 nM/18 nM/15 nM.
靶点 RSK4 RSK3 RSK2 RSK1    
IC50 15 nM 18 nM 24 nM 31 nM    

质量控制

化学结构

BI-D1870

相关生物数据

BI-D1870