EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #72712_C
90 kDa核糖体S6激酶（RSK）抑制剂
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总览
BI-D1870可抑制90 kDa核糖体S6激酶（RSK）， RSK属于丝氨酸/苏氨酸激酶家族，参与多种细胞过程，如生长、生存和迁徙（Romeo et al.）。
维持和自我更新
·减少体外神经干细胞增殖和自我更新（Karelina et al.）。
癌症研究
·抑制乳腺癌细胞系的生长（Stratford et al., Dhillon et al.）。
别名
不适用
细胞类型
癌细胞及细胞系，乳腺细胞，神经干/祖细胞
种属
人，小鼠，非人灵长类，其他物种，大鼠
研究领域
癌症，上皮细胞研究，干细胞生物学
CAS 编号
501437-28-1
化学式
C₁₉H₂₃F₂N₅O₂
分子量
391.4 g/mol
纯度
≥ 95 %
靶点
RSK
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
相关材料与文献
技术资料 (1)
文献 (5)
The selectivity of protein kinase inhibitors: a further update.
The Biochemical journal 2007 DEC
Abstract
The specificities of 65 compounds reported to be relatively specific inhibitors of protein kinases have been profiled against a panel of 70-80 protein kinases. On the basis of this information,the effects of compounds that we have studied in cells and other data in the literature,we recommend the use of the following small-molecule inhibitors: SB 203580/SB202190 and BIRB 0796 to be used in parallel to assess the physiological roles of p38 MAPK (mitogen-activated protein kinase) isoforms,PI-103 and wortmannin to be used in parallel to inhibit phosphatidylinositol (phosphoinositide) 3-kinases,PP1 or PP2 to be used in parallel with Src-I1 (Src inhibitor-1) to inhibit Src family members; PD 184352 or PD 0325901 to inhibit MKK1 (MAPK kinase-1) or MKK1 plus MKK5,Akt-I-1/2 to inhibit the activation of PKB (protein kinase B/Akt),rapamycin to inhibit TORC1 [mTOR (mammalian target of rapamycin)-raptor (regulatory associated protein of mTOR) complex],CT 99021 to inhibit GSK3 (glycogen synthase kinase 3),BI-D1870 and SL0101 or FMK (fluoromethylketone) to be used in parallel to inhibit RSK (ribosomal S6 kinase),D4476 to inhibit CK1 (casein kinase 1),VX680 to inhibit Aurora kinases,and roscovitine as a pan-CDK (cyclin-dependent kinase) inhibitor. We have also identified harmine as a potent and specific inhibitor of DYRK1A (dual-specificity tyrosine-phosphorylated and -regulated kinase 1A) in vitro. The results have further emphasized the need for considerable caution in using small-molecule inhibitors of protein kinases to assess the physiological roles of these enzymes. Despite being used widely,many of the compounds that we analysed were too non-specific for useful conclusions to be made,other than to exclude the involvement of particular protein kinases in cellular processes.
The expression of activated Y-box binding protein-1 serine 102 mediates trastuzumab resistance in breast cancer cells by increasing CD44+ cells.
Oncogene 2010 NOV
Abstract
The development of acquired resistance to trastuzumab remains a prevalent challenge in the treatment of patients whose tumors express human epidermal growth factor 2 (HER2). We previously reported that HER2 overexpressing breast cancers are dependent on Y-box binding protein-1 (YB-1) for growth and survival. As YB-1 is also linked to drug resistance in other types of cancer,we address its possible role in trastuzumab insensitivity. Employing an in vivo model of acquired resistance,we demonstrate that resistant cell lines have elevated levels of P-YB-1(S102) and its activating kinase P-RSK and these levels are sustained following trastuzumab treatment. Further,to demonstrate the importance of YB-1 in mediating drug resistance,the expression of the active mutant YB-1(S102D) rendered the BT474 cell line insensitive to trastuzumab. Questioning the role of tumor-initiating cells (TIC) and their ability to escape cancer therapies,we investigate YB-1's role in inducing the cancer stem cell marker CD44. Notably,the resistant cells express more CD44 mRNA and protein compared with BT474 cells,which correlated with increased mammosphere formation. Expression of YB-1(S102D) in the BT474 cells increase CD44 protein levels,resulting in enhanced mammosphere formation. Further,exposing BT474 cells to trastuzumab selected for a resistant sub-population enriched for CD44. Conversely,small intefering RNA inhibition of CD44 restored trastuzumab sensitivity in the resistant cell lines. Our findings provide insight on a novel mechanism employed by tumor cells to acquire the ability to escape the effects of trastuzumab and suggest that targeting YB-1 may overcome resistance by eliminating the unresponsive TIC population,rendering the cancer sensitive to therapy.
Regulation and function of the RSK family of protein kinases.
The Biochemical journal 2012 JAN
Abstract
The RSK (90 kDa ribosomal S6 kinase) family comprises a group of highly related serine/threonine kinases that regulate diverse cellular processes,including cell growth,proliferation,survival and motility. This family includes four vertebrate isoforms (RSK1,RSK2,RSK3 and RSK4),and single family member orthologues are also present in Drosophila and Caenorhabditis elegans. The RSK isoforms are downstream effectors of the Ras/ERK (extracellular-signal-regulated kinase) signalling pathway. Significant advances in the field of RSK signalling have occurred in the past few years,including several new functions ascribed to the RSK isoforms,the discovery of novel protein substrates and the implication of different RSK isoforms in cancer. Collectively,these new findings increase the diversity of biological functions regulated by RSK,and highlight potential new directions of research. In the present paper,we review the structure,expression and activation mechanisms of the RSK isoforms,and discuss their physiological roles on the basis of established substrates and recent discoveries.
更多信息
| Molecular Weight | 391.4 g/mol |
|---|---|
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
| Alternative Names | Not applicable |
| Cas Number | 501437-28-1 |
| Chemical Formula | C₁₉H₂₃F₂N₅O₂ |
| 纯度 | ≥ 95 % |
| Target | RSK |
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