BI-D1870
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BI-D1870是一种细胞可透过的p90 RSK亚型的抑制剂,对RSK1\RSK2\RSK3和RSK4的IC50值分别为31 nM\24 nM\18 nM和15 nM[1].
BI-D1870是二氢蝶啶的衍生物,是RSK亚型非常特异的抑制剂.该物质是一种ATP竞争性抑制剂.当ATP浓度为10 μM和100 μM时,BI-D1870对RSK1和RSK2的IC50值分别为5 nM\10 nM和10 nM\20 nM.当ATP为100 μM时,BI-D1870也可抑制RSK3和RSK4,IC50值分别为18 nM和15 nM.BI-D1870对RSK的抑制活性比对其他一些AGC激酶强500多倍,表明BI-D1870是RSK的特异性抑制剂.此外,BI-D1870可在Rat-2细胞中诱导ERK1/ERK2磷酸化及后续的CREB磷酸化[1].
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 391.42 |
Cas No. | 501437-28-1 |
Formula | C19H23F2N5O2 |
Solubility | insoluble in H2O; ≥19.55 mg/mL in DMSO; ≥2.5 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one |
SDF | Download SDF |
Canonical SMILES | CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
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 |
质量控制和MSDS
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