RWJ-67657featured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:510234
CAS#:215303-72-3
Description:RWJ-67657 is a potent p38 MAPK inhibitor, which inhibited the release of TNF-alpha by lipopolysaccharide (a monocyte stimulus)-treated human peripheral blood mononuclear cells with an IC(50) of 3 nM, as well as the release of TNF-alpha from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B (a T cell stimulus), with an IC(50) value of 13 nM. This compound was approximately 10-fold more potent than the literature standard p38 kinase inhibitor SB 203580 in all p38 dependent in vitro systems tested.
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Chemical Structure
Theoretical Analysis
MedKoo Cat#: 510234Name: RWJ-67657CAS#: 215303-72-3Chemical Formula: C27H24FN3OExact Mass: 425.19034Molecular Weight: 425.49736Elemental Analysis: C, 76.21; H, 5.69; F, 4.46; N, 9.88; O, 3.76
Synonym:RWJ67657; RWJ-67657; RWJ 67657
IUPAC/Chemical Name:4-(4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl)but-3-yn-1-ol
InChi Key:QSUSKMBNZQHHPA-UHFFFAOYSA-N
InChi Code:InChI=1S/C27H24FN3O/c28-24-13-11-22(12-14-24)26-27(23-15-17-29-18-16-23)31(25(30-26)10-4-5-20-32)19-6-9-21-7-2-1-3-8-21/h1-3,7-8,11-18,32H,5-6,9,19-20H2
SMILES Code:OCCC#CC1=NC(C2=CC=C(F)C=C2)=C(C3=CC=NC=C3)N1CCCC4=CC=CC=C4
Technical Data
Additional Information
References
1: Westra J, Kułdo JM, van Rijswijk MH, Molema G,Limburg PC. Chemokine production and E-selectin expression in activatedendothelial cells are inhibited by p38 MAPK (mitogen activated proteinkinase) inhibitor RWJ 67657. Int Immunopharmacol. 2005Jul;5(7-8):1259-69. Epub 2005 Apr 26. PubMed PMID: 15914330.
2: Westra J, Limburg PC, de Boer P, van Rijswijk MH. Effects of RWJ67657, a p38 mitogen activated protein kinase (MAPK) inhibitor, on theproduction of inflammatory mediators by rheumatoid synovial fibroblasts.Ann Rheum Dis. 2004 Nov;63(11):1453-9. PubMed PMID: 15479895; PubMedCentral PMCID: PMC1754789.
3: Westra J, Doornbos-van der Meer B, de Boer P, van Leeuwen MA, vanRijswijk MH, Limburg PC. Strong inhibition of TNF-alpha production andinhibition of IL-8 and COX-2 mRNA expression in monocyte-derivedmacrophages by RWJ 67657, a p38 mitogen-activated protein kinase (MAPK)inhibitor. Arthritis Res Ther. 2004;6(4):R384-92. Epub 2004 Jun 21.PubMed PMID: 15225374; PubMed Central PMCID: PMC464924.
4: Parasrampuria DA, de Boer P, Desai-Krieger D, Chow AT, Jones CR.Single-dose pharmacokinetics and pharmacodynamics of RWJ 67657, aspecific p38 mitogen-activated protein kinase inhibitor: afirst-in-human study. J Clin Pharmacol. 2003 Apr;43(4):406-13. PubMedPMID: 12723461.
5: Faas MM, Moes H, Fijen JW, Muller Kobold AC, Tulleken JE, ZijlstraJG. Monocyte intracellular cytokine production during human endotoxaemiawith or without a second in vitro LPS challenge: effect of RWJ-67657, ap38 MAP-kinase inhibitor, on LPS-hyporesponsiveness. Clin Exp Immunol.2002 Feb;127(2):337-43. PubMed PMID: 11876759; PubMed Central PMCID:PMC1906333.
6: Fijen JW, Zijlstra JG, De Boer P, Spanjersberg R, Tervaert JW, VanDer Werf TS, Ligtenberg JJ, Tulleken JE. Suppression of the clinical andcytokine response to endotoxin by RWJ-67657, a p38 mitogen-activatedprotein-kinase inhibitor, in healthy human volunteers. Clin Exp Immunol.2001 Apr;124(1):16-20. PubMed PMID: 11359438; PubMed Central PMCID:PMC1906020.
7: Wadsworth SA, Cavender DE, Beers SA, Lalan P, Schafer PH, Malloy EA,Wu W, Fahmy B, Olini GC, Davis JE, Pellegrino-Gensey JL, Wachter MP,Siekierka JJ. RWJ 67657, a potent, orally active inhibitor of p38mitogen-activated protein kinase. J Pharmacol Exp Ther. 1999Nov;291(2):680-7. PubMed PMID: 10525088.
MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(ResearchTrianglePark,简称RTP),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
中文名MedKoo中 文美帝药库医药科技公司创立于2008年总部位于美国东海岸
MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务。 MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务和分子有竞争力的价格。MedKoo是您可靠的合作伙伴采购药物发现和药物分子。 MedKoo是世界的抗癌化学试剂和激酶抑制剂供应商之一。我们制造,销售和分销用于肿瘤学研究的高质量抗癌小分子试剂。我们的使命是建立世界上全面的抗癌小分子集合。我们还为制药行业,医学研究组织和学术机构提供高质量的研究服务。我们致力于以具有竞争力的价格提供服务和分子。MedKoo是您可靠的药物发现和药物分子采购合作伙伴。 CRISPR-Cas9是近年兴起的用于靶向基因组特定位置,进行DNA修饰的重要工具。研究发现CRISPR是细菌为了应对病毒的攻击而演化而来的获得性免疫防御机制。具体来说,在CRISPR和Cas9的作用下,经由小RNA分子的引导,靶向并沉默入侵者遗传物质核酸的关键部分。在该系统中,crRNA(CRISPR-derivedRNA)与tracrRNA(trans-activatingRNA)结合形成的复合物能特异性识别靶基因序列,并引导Cas9核酸内切酶在靶定位点剪切双链DNA,随后,细胞的非同源末端连接修复机制(NHEJ)重新连接断裂处的基因组DNA,并引入插入或缺失突变。另外也可以提供一个外源双链供体DNA(Donor)通过同源重组(HR)整合进断裂处的基因组,从而达到对基因组DNA进行修饰的目的。
目前,CRISPR-Cas9系统的高效基因组编辑功能已被应用于多种生物,包括小鼠、大鼠、斑马鱼、秀丽隐杆线虫,也包含多种细菌和植物,甚至在人体上也有应用。
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