{"id":1065,"date":"2020-12-03T11:30:01","date_gmt":"2020-12-03T02:30:01","guid":{"rendered":"https:\/\/www.promega.co.jp\/resources\/faq\/?p=1065"},"modified":"2021-01-19T12:57:26","modified_gmt":"2021-01-19T03:57:26","slug":"q561","status":"publish","type":"post","link":"https:\/\/www.promega.co.jp\/resources\/faq\/reporter-signaling\/cell-signaling\/kinase-inhibitor\/mek-inhibitor-u0126\/q561","title":{"rendered":"MEK Inhibitor U0126\u3068\u306f\u3069\u306e\u3088\u3046\u306a\u3082\u306e\u3067\u3059\u304b\uff1f\u307e\u305fPD98059\u3068\u306e\u3068\u306e\u9055\u3044\u306f\uff1f"},"content":{"rendered":"\n<p>MAP\u30ad\u30ca\u30fc\u30bc\u30ad\u30ca\u30fc\u30bc1\u53ca\u30732(MEK1\/2)\u306fERK1\/2\u3092\u30ea\u30f3\u9178\u5316\u3057\u3066\u6d3b\u6027\u5316\u3055\u305b\u308b\u9175\u7d20\u3067\u3059\u3002MEK Inhibitor U0126(\u30ab\u30bf\u30ed\u30b0\u756a\u53f7V1121)\u306f\u65b0\u898f\u306eMEK1\/2\u306e\u9078\u629e\u7684\u963b\u5bb3\u5264\u3067\u3059\u3002PD098059\u3068\u540c\u3058\u304f\u3001U0126\u306fMAPK\u306e\u6d3b\u6027\u5316\u3092\u963b\u5bb3\u3057\u307e\u3059\u3002U0126\u306f\u6709\u6a5f\u5316\u5408\u7269\u306e\u4e00\u7a2e(1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene;MW= 426.5)\u3067\u3001MEK\u306b\u975e\u7af6\u5408\u7684\u306b\u7d50\u5408\u3057\u3066\u89e6\u5a92\u6d3b\u6027\u3092\u963b\u5bb3\u3059\u308b\u3053\u3068\u306b\u3088\u308a\u3001ERK\u306e\u30ea\u30f3\u9178\u5316\u306b\u3088\u308b\u6d3b\u6027\u5316\u3092\u59a8\u3052\u307e\u3059\u3002\u3057\u304b\u3082MEK1\u304a\u3088\u3073MEK2\u3092\u540c\u7b49\u306b\u963b\u5bb3\u3057\u307e\u3059\uff08in vitro\u3067MEK1\u306b\u5bfe\u3059\u308bIC<sub>50<\/sub>=72nM\u3001MEK2\u306b\u5bfe\u3059\u308bIC<sub>50<\/sub>=58nM\uff09(1-3)\u3002\u4e00\u65b9\u3001MEK inhibitor PD98059\u306f\u3001Raf\u306b\u3088\u308bMEK1\u306e\u6d3b\u6027\u5316\u3092\u59a8\u3052\u308b\u963b\u5bb3\u5264\u3067\u3059(PD98059\u306fMEK2\u306e\u963b\u5bb3\u52b9\u679c\u306f\u307b\u3068\u3093\u3069\u3042\u308a\u307e\u305b\u3093\uff1ain vitro\u3067MEK1\u306b\u5bfe\u3059\u308bIC<sub>50<\/sub>=4\u03bcM\u3001MEK2\u306b\u5bfe\u3059\u308bIC<sub>50<\/sub>=50\u03bcM)\u3002PD98059&nbsp;\u306f\u4e0d\u6d3b\u6027\u578b\u306eMEK1\u306b\u7d50\u5408\u3057\u3001Raf\u306b\u3088\u308b\u30ea\u30f3\u9178\u5316\u3092\u59a8\u3052\u307e\u3059\u3002\u3057\u304b\u3057\u3001\u3059\u3067\u306b\u6d3b\u6027\u5316\u3057\u3066\u3044\u308bMEK1\u306b\u306f\u307b\u3068\u3093\u3069\u4f5c\u7528\u3057\u307e\u305b\u3093\u3002\u3064\u307e\u308a\u3001U0126\u306fMEK1\/2\u306e\u6d3b\u6027\u72b6\u614b\u306b\u3088\u3089\u305a\u3001ERK1\/2\u306e\u6d3b\u6027\u5316\u306e\u4e0b\u6d41\u306b\u3042\u308b\u9175\u7d20\u306e\u6d3b\u6027\u5316\u3092\u963b\u5bb3\u3057\u307e\u3059\u3002\u3055\u3089\u306b\u3001U0126\u306fPD98059\u3088\u308a\u3082in vitro\u304a\u3088\u3073in vivo\u306e\u4e21\u65b9\u3067\u9ad8\u3044\u963b\u5bb3\u52b9\u679c\u3092\u793a\u3057\u307e\u3059\u3002\u7d30\u80de\u5185\u3067U0126\u306fIC<sub>50<\/sub>\u50240.07\u03bcM\u3067\u5b89\u5b9a\u306b\u6d3b\u6027\u578bMEK2\u3092\u963b\u5bb3\u3057\u307e\u3059\u3002\u4e00\u65b9\u3001PD98059\u306eIC<sub>50<\/sub>\u5024\u306f5.00\u03bcM\u3088\u308a\u3082\u5927\u304d\u304f\u306a\u308a\u307e\u3059\u3002IC<sub>50<\/sub>\u5024\u306f\u30ad\u30ca\u30fc\u30bc\u306e\u7a2e\u985e\u3084\u7d30\u80de\u7a2e\u306b\u3088\u3063\u3066\u305d\u308c\u305e\u308c\u7570\u306a\u308a\u307e\u3059\u3002(PN76-Q&amp;A)(eNotes-FAQ0005)<\/p>\n\n\n\n<p><strong>\u53c2\u8003<\/strong><strong>\u6587\u732e:<\/strong><\/p>\n\n\n\n<ol><li>Dudley, D.T. et al. (1995) A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc. Natl. Acad. Sci. USA 92, 7686.<\/li><li>Alessi, D.R. et al. (1995) PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J. Biol. Chem. 270, 27489.<\/li><li>Favata, M.F. et al. (1998) Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J. Biol. Chem. 273, 18623.<\/li><\/ol>\n","protected":false},"excerpt":{"rendered":"<p>MAP\u30ad\u30ca\u30fc\u30bc\u30ad\u30ca\u30fc\u30bc1\u53ca\u30732(MEK1\/2)\u306fERK1\/2\u3092\u30ea\u30f3\u9178\u5316\u3057\u3066\u6d3b\u6027\u5316\u3055\u305b\u308b\u9175\u7d20\u3067\u3059\u3002MEK Inhibitor U0126(\u30ab\u30bf\u30ed\u30b0\u756a\u53f7V1121)\u306f\u65b0\u898f\u306eMEK1\/2\u306e\u9078\u629e\u7684\u963b\u5bb3\u5264\u3067\u3059\u3002PD098059\u3068\u540c &#8230; <\/p>\n","protected":false},"author":16,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":[],"categories":[206],"tags":[],"_links":{"self":[{"href":"https:\/\/www.promega.co.jp\/resources\/faq\/wp-json\/wp\/v2\/posts\/1065"}],"collection":[{"href":"https:\/\/www.promega.co.jp\/resources\/faq\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.promega.co.jp\/resources\/faq\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.promega.co.jp\/resources\/faq\/wp-json\/wp\/v2\/users\/16"}],"replies":[{"embeddable":true,"href":"https:\/\/www.promega.co.jp\/resources\/faq\/wp-json\/wp\/v2\/comments?post=1065"}],"version-history":[{"count":1,"href":"https:\/\/www.promega.co.jp\/resources\/faq\/wp-json\/wp\/v2\/posts\/1065\/revisions"}],"predecessor-version":[{"id":1066,"href":"https:\/\/www.promega.co.jp\/resources\/faq\/wp-json\/wp\/v2\/posts\/1065\/revisions\/1066"}],"wp:attachment":[{"href":"https:\/\/www.promega.co.jp\/resources\/faq\/wp-json\/wp\/v2\/media?parent=1065"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.promega.co.jp\/resources\/faq\/wp-json\/wp\/v2\/categories?post=1065"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.promega.co.jp\/resources\/faq\/wp-json\/wp\/v2\/tags?post=1065"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}