EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #72682_C
p38 MAPK抑制剂
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总览
BIRB-796是一种高效的p38 MAPK抑制剂（Kd = 0.1 nM），可阻断LPS刺激的THP-1细胞中TNFα的释放（IC50 = 18 nM）（Pargellis et al.）。在10 μM浓度时，BIRB-796也能体外抑制JNK2α2，但在较低浓度时，BIRB-796能抑制p38 MAPK，而不影响JNK底物的磷酸化(Bain et al.; Kuma et al.)。
维持和自我更新
·恢复老年小鼠肌肉卫星细胞的自我更新能力（Bernet et al.）。
·增加水凝胶中培养的功能性老年骨骼肌干细胞的再生能力（Cosgrove et al.）。
·阻断GADD45G诱导的长期再生造血干细胞的分化（Thalheimer et al.）。
·在添加SCF、TPO和FLT3L的无血清培养基中，增强脐带血来源的造血干细胞的活性（Baudet et al.）。
·抑制myocilin对人间充质干细胞的成骨分化（Kwon et al.）。
细胞类型
造血干/祖细胞，间充质干/祖细胞，肌源干/祖细胞
种属
人，小鼠，非人灵长类，其他物种，大鼠
应用
扩增，培养
研究领域
干细胞生物学
CAS 编号
285983-48-4
化学式
C₃₁H₃₇N₅O₃
纯度
≥98%
通路
p38 MAPK
靶点
p38 MAPK
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。
应用领域
本产品专为以下研究领域设计，适用于工作流程中的高亮阶段。探索这些工作流程，了解更多我们为各研究领域提供的其他配套产品。
相关材料与文献
技术资料 (3)
文献 (8)
Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site.
Nature structural biology 2002 APR
Abstract
The p38 MAP kinase plays a crucial role in regulating the production of proinflammatory cytokines,such as tumor necrosis factor and interleukin-1. Blocking this kinase may offer an effective therapy for treating many inflammatory diseases. Here we report a new allosteric binding site for a diaryl urea class of highly potent and selective inhibitors against human p38 MAP kinase. The formation of this binding site requires a large conformational change not observed previously for any of the protein Ser/Thr kinases. This change is in the highly conserved Asp-Phe-Gly motif within the active site of the kinase. Solution studies demonstrate that this class of compounds has slow binding kinetics,consistent with the requirement for conformational change. Improving interactions in this allosteric pocket,as well as establishing binding interactions in the ATP pocket,enhanced the affinity of the inhibitors by 12,000-fold. One of the most potent compounds in this series,BIRB 796,has picomolar affinity for the kinase and low nanomolar inhibitory activity in cell culture.
BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo.
The Journal of biological chemistry 2005 MAY
Abstract
The compound BIRB796 inhibits the stress-activated protein kinases p38alpha and p38beta and is undergoing clinical trials for the treatment of inflammatory diseases. Here we report that BIRB796 also inhibits the activity and the activation of SAPK3/p38gamma. This occurs at higher concentrations of BIRB796 than those that inhibit p38alpha and p38beta and at lower concentrations than those that inhibit the activation of JNK isoforms. We also show that at these concentrations,BIRB796 blocks the stress-induced phosphorylation of the scaffold protein SAP97,further establishing that this is a physiological substrate of SAPK3/p38gamma. Our results demonstrate that BIRB796,in combination with SB203580,a compound that inhibits p38alpha and p38beta,but not the other p38 isoforms,can be used to identify physiological substrates of SAPK3/p38gamma as well as those of p38alpha and p38beta.
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.
更多信息
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
|---|---|
| Cas Number | 285983-48-4 |
| Chemical Formula | C₃₁H₃₇N₅O₃ |
| 纯度 | ≥ 98% |
| Target | p38 MAPK |
| Pathway | p38 MAPK |
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