![]() 6-(4-氟苯基)-5-(4-吡啶基)-2,3-二氢咪唑并[2,1-B]-噻唑结构式
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常用名 | 6-(4-氟苯基)-5-(4-吡啶基)-2,3-二氢咪唑并[2,1-B]-噻唑 | 英文名 | SKF 86002 |
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CAS号 | 72873-74-6 | 分子量 | 297.350 | |
密度 | 1.4±0.1 g/cm3 | 沸点 | 476.1±55.0 °C at 760 mmHg | |
分子式 | C16H12FN3S | 熔点 | 189-190ºC(lit.) | |
MSDS | 美版 | 闪点 | 241.7±31.5 °C |
The discovery of novel chemotypes of p38 kinase inhibitors.
Curr. Top. Med. Chem 5(10) , 953-65, (2005) In the late 1970s and the early 1980s the initial p38 chemotype, the triaryl imidazoles, was discovered as an off-target effect during the development of cyclooxygenase and 5-lipoxygenase inhibitors long before the identity of the p38 kinase was known. During... |
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Activation of p38MAPK contributes to expanded polyglutamine-induced cytotoxicity.
PLoS ONE 3(5) , e2130, (2008) The signaling pathways that may modulate the pathogenesis of diseases induced by expanded polyglutamine proteins are not well understood.Herein we demonstrate that expanded polyglutamine protein cytotoxicity is mediated primarily through activation of p38MAPK... |
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Differential activation of the c-Jun N-terminal kinase pathway in arsenite-induced apoptosis and sensitization of chemically resistant compared to susceptible B-lymphoma cell lines.
Toxicol. Sci. 68(1) , 82-92, (2002) Various forms of inorganic arsenic are significant environmental contaminants that have multiple effects on cells, including the induction of apoptotic cell death. Induction of apoptosis in lymphoid cells can mediate immunotoxicity following exposure to chemi... |
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A Biacore biosensor method for detailed kinetic binding analysis of small molecule inhibitors of p38alpha mitogen-activated protein kinase.
Anal. Biochem. 325(1) , 126-36, (2004) Protein kinases are emerging as one of the most intensely studied classes of enzymes as their central roles in physiologically and clinically important cellular signaling events become more clearly understood. We report here the development of a real-time, la... |
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Lipopolysaccharide: a p38 MAPK-dependent disrupter of neutrophil chemotaxis.
Microcirculation 12(5) , 421-32, (2005) In sepsis, and in models of sepsis including endotoxemia, impaired neutrophil recruitment and chemotaxis have been reported. The inability of the endotoxemic neutrophil to chemotax could be attributed to the fact that intracellular signaling via LPS overrides... |
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High-throughput RT-PCR analysis of multiple transcripts using a microplate RNA isolation procedure.
Biotechniques 22(6) , 1107-13, (1997) We have developed a high-throughput, multiplex reverse transcription PCR (RTPCR) assay that is suitable for the analysis of medium-to low-copy cellular RNA transcripts from small numbers of cells (10(4)). High throughput was attained by utilizing microplate-b... |
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The effects of a cytokine suppressive anti-inflammatory drug on the output of prostaglandin E(2) and interleukin-1 beta from human fetal membranes.
Mol. Hum. Reprod. 8(3) , 281-5, (2002) Fetal membranes are a primary source of prostaglandins and pro-inflammatory cytokines implicated in human parturition, so the inhibition of inflammatory pathways may be of benefit in pregnancies complicated by premature labour. We have therefore investigated ... |
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p38 MAP kinase negatively regulates angiotensin II-mediated effects on cell cycle molecules in human coronary smooth muscle cells.
Biochem. Biophys. Res. Commun. 305(3) , 552-6, (2003) Many of the signaling events in VSMC stimulated by angiotensin II (AngII) are mediated by members of the mitogen-activated protein kinase (MAPK) family, including p38 MAPK. The role of p38 MAPK in AngII-mediated cell cycle regulation is poorly understood. The... |
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Low density lipoproteins inhibit the Na+/H+ antiport in human platelets via activation of p38MAP kinase.
Biochem. Biophys. Res. Commun. 340(3) , 751-7, (2006) Low density lipoproteins (LDL) inhibit the Na+/H+ antiport and thereby sensitize platelet towards agonist. However, mechanisms underlying the suppressing effect of LDL on Na+/H+ exchange are unclear. We here show that the lowering of intracellular pH and the ... |
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Integrin alpha2beta1 mediates isoform-specific activation of p38 and upregulation of collagen gene transcription by a mechanism involving the alpha2 cytoplasmic tail.
J. Cell Biol. 147 , 401-16, (1999) Two collagen receptors, integrins alpha1beta1 and alpha2beta1, can regulate distinct functions in cells. Ligation of alpha1beta1, unlike alpha2beta1, has been shown to result in recruitment of Shc and activation of the Ras/ERK pathway. To identify the downstr... |